Home Epigenetics HDAC inhibitor - Autophagy activator - Apoptosis related activator Entinostat (MS-275) For research use only.

Entinostat (MS-275)

Synonyms: SNDX-275

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.

Entinostat (MS-275) Chemical Structure

Entinostat (MS-275) Chemical Structure

CAS: 209783-80-2

Selleck's Entinostat (MS-275) has been cited by 397 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

Products often used together with Entinostat (MS-275)

Vorinostat (SAHA)

Entinostat and Vorinostat demonstrate activated HIV production in latently infected primary T cells.

Wightman F, et al. AIDS. 2013 Nov 28; 27(18): 2853–2862.

Panobinostat (LBH589)

Entinostat and Panobinostat can downregulate the expression of selected HR genes in HR-proficient human ovarian cancer cells.

Quisinostat (JNJ-26481585) 2HCl

Entinostat and Quisinostat 2HCl are HDAC inhibitors that prevent CaMKII overexpression-induced cardiac myocyte hypertrophy.

Zhang M, et al. J Mol Cell Cardiol. 2020 Dec;149:73-81.

Exemestane

Entinostat and Exemestane give a significant improvement in progression-free survival and overall survival in advanced HR-positive, HER2-negative breast cancer.

Connolly RM, et al. J Clin Oncol. 2021 Oct 1;39(28):3171-3181.

Decitabine

Entinostat and Decitabine induce apoptosis in J82, J82CisR, and RT-112 cells and cell cycle arrest in J82 and RT-112 cell lines.

Wang C, et al. Cancers (Basel). 2020 Feb 3;12(2):337.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCC-3 Growth Inhibition Assay IC50=0.061 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.06355 μM SANGER
697 Growth Inhibition Assay IC50=0.09976 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=0.10334 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.10912 μM SANGER
ES1 Growth Inhibition Assay IC50=0.11255 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=0.11579 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=0.12974 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.13527 μM SANGER
CRO-AP2 Growth Inhibition Assay IC50=0.16889 μM SANGER
A3-KAW Growth Inhibition Assay IC50=0.17627 μM SANGER
SF539 Growth Inhibition Assay IC50=0.19593 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.19619 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.20113 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.22959 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.24079 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.27833 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.28708 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.30256 μM SANGER
ATN-1 Growth Inhibition Assay IC50=0.30576 μM SANGER
HEL Growth Inhibition Assay IC50=0.31348 μM SANGER
NB12 Growth Inhibition Assay IC50=0.31756 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.3351 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.33716 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.3381 μM SANGER
SR Growth Inhibition Assay IC50=0.34261 μM SANGER
CMK Growth Inhibition Assay IC50=0.35727 μM SANGER
ES8 Growth Inhibition Assay IC50=0.36022 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=0.3673 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.36935 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.37121 μM SANGER
DEL Growth Inhibition Assay IC50=0.37487 μM SANGER
ARH-77 Growth Inhibition Assay IC50=0.38193 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.38649 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=0.38701 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=0.38776 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.39868 μM SANGER
CHP-126 Growth Inhibition Assay IC50=0.40231 μM SANGER
A101D Growth Inhibition Assay IC50=0.403 μM SANGER
SCH Growth Inhibition Assay IC50=0.40342 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.40367 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.40613 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.41017 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=0.4112 μM SANGER
OPM-2 Growth Inhibition Assay IC50=0.41513 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=0.43153 μM SANGER
BC-1 Growth Inhibition Assay IC50=0.43403 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=0.43453 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=0.43897 μM SANGER
LS-513 Growth Inhibition Assay IC50=0.44501 μM SANGER
K5 Growth Inhibition Assay IC50=0.47025 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.48358 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=0.49227 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.49661 μM SANGER
HC-1 Growth Inhibition Assay IC50=0.50473 μM SANGER
ACN Growth Inhibition Assay IC50=0.51028 μM SANGER
HCC1599 Growth Inhibition Assay IC50=0.5157 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.53041 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=0.53663 μM SANGER
HL-60 Growth Inhibition Assay IC50=0.54261 μM SANGER
NB17 Growth Inhibition Assay IC50=0.5438 μM SANGER
TE-1 Growth Inhibition Assay IC50=0.55306 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=0.55401 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=0.56105 μM SANGER
L-363 Growth Inhibition Assay IC50=0.56657 μM SANGER
BL-41 Growth Inhibition Assay IC50=0.56889 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.57073 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.57848 μM SANGER
ONS-76 Growth Inhibition Assay IC50=0.58242 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=0.58504 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.58703 μM SANGER
NB69 Growth Inhibition Assay IC50=0.59825 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=0.60719 μM SANGER
LU-165 Growth Inhibition Assay IC50=0.61812 μM SANGER
LOUCY Growth Inhibition Assay IC50=0.63364 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=0.63541 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.64276 μM SANGER
NALM-6 Growth Inhibition Assay IC50=0.6486 μM SANGER
CW-2 Growth Inhibition Assay IC50=0.65794 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=0.65947 μM SANGER
NB13 Growth Inhibition Assay IC50=0.66817 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.68343 μM SANGER
ECC12 Growth Inhibition Assay IC50=0.70086 μM SANGER
KALS-1 Growth Inhibition Assay IC50=0.70492 μM SANGER
COR-L279 Growth Inhibition Assay IC50=0.70996 μM SANGER
NB14 Growth Inhibition Assay IC50=0.72617 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=0.74661 μM SANGER
SW954 Growth Inhibition Assay IC50=0.75999 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=0.77348 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.77567 μM SANGER
Daudi Growth Inhibition Assay IC50=0.77681 μM SANGER
BC-3 Growth Inhibition Assay IC50=0.78308 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.7836 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.80147 μM SANGER
CPC-N Growth Inhibition Assay IC50=0.80524 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=0.81084 μM SANGER
CESS Growth Inhibition Assay IC50=0.81197 μM SANGER
LC4-1 Growth Inhibition Assay IC50=0.84007 μM SANGER
BL-70 Growth Inhibition Assay IC50=0.85702 μM SANGER
ES4 Growth Inhibition Assay IC50=0.85868 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.87171 μM SANGER
JAR Growth Inhibition Assay IC50=0.87827 μM SANGER
ST486 Growth Inhibition Assay IC50=0.87917 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.88096 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.88687 μM SANGER
EHEB Growth Inhibition Assay IC50=0.92585 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=0.93284 μM SANGER
GOTO Growth Inhibition Assay IC50=0.95076 μM SANGER
LXF-289 Growth Inhibition Assay IC50=0.95901 μM SANGER
ES6 Growth Inhibition Assay IC50=0.96437 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=0.9683 μM SANGER
DMS-153 Growth Inhibition Assay IC50=0.97469 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=0.97831 μM SANGER
HH Growth Inhibition Assay IC50=0.98959 μM SANGER
SH-4 Growth Inhibition Assay IC50=1.0241 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=1.03454 μM SANGER
TGW Growth Inhibition Assay IC50=1.07675 μM SANGER
L-540 Growth Inhibition Assay IC50=1.10604 μM SANGER
PF-382 Growth Inhibition Assay IC50=1.11513 μM SANGER
LC-1F Growth Inhibition Assay IC50=1.12007 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=1.13165 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=1.15364 μM SANGER
HCC2218 Growth Inhibition Assay IC50=1.16641 μM SANGER
HAL-01 Growth Inhibition Assay IC50=1.16943 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=1.17659 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=1.17898 μM SANGER
EVSA-T Growth Inhibition Assay IC50=1.18114 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.20266 μM SANGER
OCUB-M Growth Inhibition Assay IC50=1.21489 μM SANGER
MEG-01 Growth Inhibition Assay IC50=1.22118 μM SANGER
no-10 Growth Inhibition Assay IC50=1.23112 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=1.24721 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=1.24776 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=1.26478 μM SANGER
CTV-1 Growth Inhibition Assay IC50=1.27425 μM SANGER
NB1 Growth Inhibition Assay IC50=1.27732 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=1.28462 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=1.28577 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=1.28663 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=1.28866 μM SANGER
LP-1 Growth Inhibition Assay IC50=1.29947 μM SANGER
LS-411N Growth Inhibition Assay IC50=1.30998 μM SANGER
CAL-148 Growth Inhibition Assay IC50=1.32542 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=1.34502 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=1.3539 μM SANGER
NCI-H2107 Growth Inhibition Assay IC50=1.35883 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=1.38978 μM SANGER
K-562 Growth Inhibition Assay IC50=1.39219 μM SANGER
PSN1 Growth Inhibition Assay IC50=1.42287 μM SANGER
HCC2157 Growth Inhibition Assay IC50=1.42691 μM SANGER
SBC-1 Growth Inhibition Assay IC50=1.42741 μM SANGER
MC116 Growth Inhibition Assay IC50=1.43615 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=1.45358 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=1.47103 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=1.47987 μM SANGER
BT-474 Growth Inhibition Assay IC50=1.51764 μM SANGER
A388 Growth Inhibition Assay IC50=1.51945 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=1.5226 μM SANGER
COLO-829 Growth Inhibition Assay IC50=1.53564 μM SANGER
KM-H2 Growth Inhibition Assay IC50=1.5667 μM SANGER
GR-ST Growth Inhibition Assay IC50=1.5682 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=1.60144 μM SANGER
KG-1 Growth Inhibition Assay IC50=1.61901 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=1.63406 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=1.63459 μM SANGER
KM12 Growth Inhibition Assay IC50=1.647 μM SANGER
NB5 Growth Inhibition Assay IC50=1.65677 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=1.68281 μM SANGER
KU812 Growth Inhibition Assay IC50=1.69605 μM SANGER
DB Growth Inhibition Assay IC50=1.70353 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=1.75234 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=1.77207 μM SANGER
ETK-1 Growth Inhibition Assay IC50=1.78879 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=1.79388 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=1.79508 μM SANGER
ES7 Growth Inhibition Assay IC50=1.80302 μM SANGER
SW872 Growth Inhibition Assay IC50=1.81395 μM SANGER
TK10 Growth Inhibition Assay IC50=1.83108 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=1.83563 μM SANGER
TE-9 Growth Inhibition Assay IC50=1.84422 μM SANGER
MLMA Growth Inhibition Assay IC50=1.88234 μM SANGER
D-542MG Growth Inhibition Assay IC50=1.89373 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.9272 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=1.9328 μM SANGER
GB-1 Growth Inhibition Assay IC50=1.93866 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=2.00262 μM SANGER
LAN-6 Growth Inhibition Assay IC50=2.01966 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=2.04502 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=2.05124 μM SANGER
HT Growth Inhibition Assay IC50=2.10454 μM SANGER
RL95-2 Growth Inhibition Assay IC50=2.11482 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=2.11792 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=2.16873 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=2.21723 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=2.26902 μM SANGER
DG-75 Growth Inhibition Assay IC50=2.27148 μM SANGER
ML-2 Growth Inhibition Assay IC50=2.32855 μM SANGER
SF126 Growth Inhibition Assay IC50=2.33094 μM SANGER
MPP-89 Growth Inhibition Assay IC50=2.33145 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=2.33277 μM SANGER
LS-123 Growth Inhibition Assay IC50=2.34936 μM SANGER
NB10 Growth Inhibition Assay IC50=2.41092 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=2.42267 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=2.4777 μM SANGER
L-428 Growth Inhibition Assay IC50=2.48521 μM SANGER
DMS-79 Growth Inhibition Assay IC50=2.54103 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=2.67562 μM SANGER
KGN Growth Inhibition Assay IC50=2.76876 μM SANGER
EW-1 Growth Inhibition Assay IC50=2.77083 μM SANGER
U-266 Growth Inhibition Assay IC50=2.84823 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=2.85641 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=2.87711 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=2.9248 μM SANGER
GI-1 Growth Inhibition Assay IC50=2.92957 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=3.00511 μM SANGER
NCI-H2227 Growth Inhibition Assay IC50=3.02079 μM SANGER
U-87-MG Growth Inhibition Assay IC50=3.03513 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=3.05206 μM SANGER
CTB-1 Growth Inhibition Assay IC50=3.05376 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=3.14378 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=3.16566 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=3.18279 μM SANGER
TE-5 Growth Inhibition Assay IC50=3.21342 μM SANGER
UACC-257 Growth Inhibition Assay IC50=3.43659 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=3.45227 μM SANGER
MFH-ino Growth Inhibition Assay IC50=3.46589 μM SANGER
SF268 Growth Inhibition Assay IC50=3.48174 μM SANGER
TE-12 Growth Inhibition Assay IC50=3.51699 μM SANGER
NB6 Growth Inhibition Assay IC50=3.55563 μM SANGER
DJM-1 Growth Inhibition Assay IC50=3.59899 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=3.61624 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=3.62671 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=3.70947 μM SANGER
RKO Growth Inhibition Assay IC50=3.77189 μM SANGER
ECC4 Growth Inhibition Assay IC50=3.97195 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=3.97547 μM SANGER
EB-3 Growth Inhibition Assay IC50=3.99633 μM SANGER
SHP-77 Growth Inhibition Assay IC50=4.00524 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=4.05625 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=4.06399 μM SANGER
MN-60 Growth Inhibition Assay IC50=4.1087 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=4.13405 μM SANGER
LU-65 Growth Inhibition Assay IC50=4.15332 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=4.18333 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=4.31432 μM SANGER
GT3TKB Growth Inhibition Assay IC50=4.33268 μM SANGER
Becker Growth Inhibition Assay IC50=4.37312 μM SANGER
HCC1187 Growth Inhibition Assay IC50=4.89657 μM SANGER
D-502MG Growth Inhibition Assay IC50=5.00416 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=5.13778 μM SANGER
NB7 Growth Inhibition Assay IC50=5.14112 μM SANGER
SW962 Growth Inhibition Assay IC50=5.38814 μM SANGER
no-11 Growth Inhibition Assay IC50=5.76343 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=5.90694 μM SANGER
COLO-684 Growth Inhibition Assay IC50=5.99494 μM SANGER
D-263MG Growth Inhibition Assay IC50=6.08895 μM SANGER
EW-24 Growth Inhibition Assay IC50=6.2851 μM SANGER
TE-10 Growth Inhibition Assay IC50=6.42623 μM SANGER
EKVX Growth Inhibition Assay IC50=6.46321 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=6.67557 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=6.92301 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=8.13166 μM SANGER
COLO-668 Growth Inhibition Assay IC50=8.27786 μM SANGER
EW-12 Growth Inhibition Assay IC50=8.40803 μM SANGER
A253 Growth Inhibition Assay IC50=8.84661 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=8.89319 μM SANGER
Calu-6 Growth Inhibition Assay IC50=8.99042 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=9.17746 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=9.77478 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=9.97904 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=10.2834 μM SANGER
GCIY Growth Inhibition Assay IC50=10.5924 μM SANGER
TE-15 Growth Inhibition Assay IC50=11.6004 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=11.7682 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=11.7786 μM SANGER
EW-3 Growth Inhibition Assay IC50=12.2463 μM SANGER
CAS-1 Growth Inhibition Assay IC50=12.3631 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=12.6131 μM SANGER
D-247MG Growth Inhibition Assay IC50=12.7952 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=12.8013 μM SANGER
LS-1034 Growth Inhibition Assay IC50=14.3975 μM SANGER
EW-18 Growth Inhibition Assay IC50=14.448 μM SANGER
Raji Growth Inhibition Assay IC50=14.5049 μM SANGER
D-283MED Growth Inhibition Assay IC50=14.6271 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=14.9696 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=15.4633 μM SANGER
P30-OHK Growth Inhibition Assay IC50=17.7831 μM SANGER
RXF393 Growth Inhibition Assay IC50=19.0186 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=20.6703 μM SANGER
U-698-M Growth Inhibition Assay IC50=20.7075 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=20.7223 μM SANGER
SW684 Growth Inhibition Assay IC50=21.1716 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=21.3154 μM SANGER
JVM-2 Growth Inhibition Assay IC50=21.4133 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=22.4148 μM SANGER
CA46 Growth Inhibition Assay IC50=31.6936 μM SANGER
SNB75 Growth Inhibition Assay IC50=33.6503 μM SANGER
KNS-42 Growth Inhibition Assay IC50=35.9624 μM SANGER
TUR Growth Inhibition Assay IC50=36.0521 μM SANGER
REH Growth Inhibition Assay IC50=37.8211 μM SANGER
EW-22 Growth Inhibition Assay IC50=42.2885 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=42.7853 μM SANGER
ES3 Growth Inhibition Assay IC50=43.1339 μM SANGER
EW-11 Growth Inhibition Assay IC50=44.8218 μM SANGER
RH-1 Growth Inhibition Assay IC50=47.5812 μM SANGER
HepG2 Function assay Inhibition of human HepG2 cells, IC50 = 0.0009 μM. 18247554
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 22705022
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 22705022
HEK293 Function assay Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells, IC50 = 0.12 μM. 19441846
HEK293 Function assay Inhibition of HDAC1 in HEK293 cells, IC50 = 0.12 μM. 18308563
SNU16 Function assay Inhibition of HDAC from human SNU16 cells, IC50 = 0.233 μM. 18247554
HEK293 Function assay Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells, IC50 = 0.25 μM. 19441846
U937 Function assay Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay, IC50 = 0.3 μM. 18381238
SK-N-BE(2) Antiproliferative assay 48 hrs Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.33 μM. 28511906
AGS Antiproliferative assay 72 hrs Antiproliferative activity against human AGS cells after 72 hrs by MTT assay, IC50 = 0.34 μM. 29787262
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay, IC50 = 0.35 μM. 26613635
HEK293 Function assay Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells, IC50 = 0.4 μM. 19441846
HEK293 Function assay Inhibition of HDAC3 in HEK293 cells, IC50 = 0.4 μM. 18308563
HEL Function assay 3 hrs Inhibition of class 1 HDAC in HEL cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.43 μM. 28511906
PC3 Growth inhibition assay 48 hrs Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay, GI50 = 0.43 μM. 28395150
HEL Antiproliferative assay 72 hrs Antiproliferative activity against human HEL cells after 72 hrs by MTT assay, IC50 = 0.44 μM. 29787262
MOLT4 Antiproliferative assay 72 hrs Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay, IC50 = 0.45 μM. 29787262
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay, IC50 = 0.47 μM. 29202397
HEL Antiproliferative assay 48 hrs Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 0.48 μM. 28511906
HCT116 Function assay Inhibition of human HCT116 cells, IC50 = 0.5 μM. 18247554
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay, IC50 = 0.55 μM. 25953722
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.55 μM. 25874326
HCT116 Growth inhibition assay 2 days Growth inhibition of human HCT116 cells after 2 days by MTT assay, GI50 = 0.6 μM. 22541394
HL60 Function assay 3 hrs Inhibition of class 1 HDAC in human HL60 cells using Boc-Ac-Lys-AMC as substrate incubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.62 μM. 28415009
MOLT4 Antiproliferative assay 48 hrs Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.65 μM. 28511906
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells, IC50 = 0.67 μM. 21742496
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.67 μM. 21650221
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 0.7 μM. 19441846
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay, IC50 = 0.7 μM. 18370373
HEK293T Function assay 1 hr Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 0.74 μM. 29289885
ML1 Antitumor assay Antitumor activity against mouse ML1 cells, IC50 = 0.75 μM. 19534534
HCT116 Antiproliferative assay 3 days Antiproliferative activity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.76 μM. 22321215
U937 Antiproliferative assay 48 hrs Antiproliferative activity against human U937 cells after 48 hrs by MTT assay, IC50 = 0.77 μM. 28415009
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.78 μM. 25874326
K562 Function assay 10 mins Inhibition of KDAC3 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 0.79 μM. 26681404
HCT116 Cytotoxicity assay 3 days Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.8 μM. 20452226
SKBR3 Antiproliferative assay Antiproliferative activity against human SKBR3 cells, IC50 = 0.87 μM. 18247554
Sf9 Function assay 3 hrs Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method, IC50 = 0.9 μM. 28501514
S2 Function assay Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.94 μM. 19317450
HEK293T Function assay 1 hr Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.07 μM. 29289885
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.2 μM. 19441846
A549 Antiproliferative assay Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay, IC50 = 1.2 μM. 18370373
HEK293T Function assay 1 hr Inhibition of human FLAG-tagged HDAC3 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.23 μM. 29289885
HEL Antiproliferative assay 48 hrs Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 1.29 μM. 28415009
G401 Antiproliferative assay 72 hrs Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.3 μM. 19441846
G401 Antiproliferative assay Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay, IC50 = 1.3 μM. 18370373
Sf9 Function assay 3 hrs Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM SAHA by f, IC50 = 1.3 μM. 28501514
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.32 μM. 28511906
Huh7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 1.4 μM. 25490700
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.41 μM. 28395150
K562 Function assay 10 mins Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 1.48 μM. 26681404
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 1.52 μM. 28415009
HeLa Antiproliferative assay Antiproliferative activity against HeLa cells by alamar blue assay, IC50 = 1.58489 μM. 17606370
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay, IC50 = 1.6 μM. 29202397
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.68 μM. 28415009
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.8 μM. 19441846
HeLa Antiproliferative assay Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay, IC50 = 1.8 μM. 18370373
HCT116 Function assay 18 hrs Inhibition of HDAC in human HCT116 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 1.96 μM. 28340413
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by MTT assay, IC50 = 2 μM. 19131248
K562 Function assay Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells., IC50 = 2 μM. 12419380
K562 Function assay Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells, IC50 = 2 μM. 14592473
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.03 μM. 28340413
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.07 μM. 28415009
NCI-H661 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 2.19 μM. 25874326
NCI-H661 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay, IC50 = 2.19 μM. 25953722
SNU-16 Function assay Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells, IC50 = 2.19459 μM. 14667227
Sf9 Function assay 17 hrs Inhibition of His6-tagged HDAC3/SMRT (395 to 489 residues) (unknown origin) co-expressed in baculovirus infected sf9 cells using (FAM)-labeled acetylated peptide substrate after 17 hrs by caliper microfluidic mobility shift assay, IC50 = 2.31206 μM. 30179749
ACHN Antiproliferative assay 72 hrs Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2.4 μM. 29787262
SGC7901 Growth inhibition assay 72 hrs Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 2.5 μM. 23061376
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 2.55 μM. 29787262
MDA-MB-231 Anticancer assay 72 hrs Anticancer activity against human MDA-MB-231 cells after 72 hrs by MTT assay, GI = 2.8 μM. 21741834
A2780 Antiproliferative assay 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 3 μM. 19441846
A2780 Antiproliferative assay Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay, IC50 = 3 μM. 18370373
HCT116 Anticancer assay 72 hrs Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, GI = 3.1 μM. 21741834
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 3.1 μM. 29787262
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 3.11 μM. 28340413
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 3.134 μM. 26140961
A2780 Function assay 18 hrs Inhibition of HDAC in human A2780 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 3.15 μM. 28340413
SW620 Function assay Inhibition of human SW620 cells, IC50 = 3.2 μM. 18247554
HeLa Function assay 30 mins Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay, IC50 = 3.2 μM. 21889343
A549 Antiproliferative assay Antiproliferative activity against human A549 cells, IC50 = 3.58 μM. 18247554
K562 Antiproliferative assay 72 hrs Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 3.66 μM. 29787262
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay, IC50 = 3.67 μM. 29202397
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 4.02 μM. 28340413
MKN45 Antiproliferative assay Antiproliferative activity against human MKN45 cells, IC50 = 4.16 μM. 18247554
MCF7 Function assay Inhibition of human MCF7 cells, IC50 = 4.3 μM. 18247554
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 4.53 μM. 28340413
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 4.63 μM. 25874326
K562 Function assay Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells., IC50 = 4.8 μM. 10425110
HeLa Function assay Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation, IC50 = 4.8 μM. 19534534
MGC803 Antiproliferative assay 72 hrs Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay, IC50 = 4.89 μM. 29202397
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 4.89 μM. 28511906
HuH7 Cytotoxicity assay 3 days Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 5.1 μM. 25490700
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 5.1 μM. 26140961
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 5.41 μM. 25874326
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay, IC50 = 5.41 μM. 25953722
A2780 Anticancer assay 72 hrs Anticancer activity against human A2780 cells after 72 hrs by MTT assay, GI = 5.7 μM. 21741834
A549 Growth inhibition assay 48 hrs Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay, GI50 = 5.76 μM. 28395150
A2780 Antiproliferative assay 48 hrs Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay, IC50 = 5.89 μM. 28340413
SMMC7721 Antiproliferative assay 72 hrs Antiproliferative activity against human SMMC7721 cells after 72 hrs by CCK-8 assay, IC50 = 5.97 μM. 29202397
U266 Antiproliferative assay 48 hrs Antiproliferative activity against human U266 cells after 48 hrs by MTT assay, IC50 = 6.1 μM. 28415009
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 6.36 μM. 28340413
U251 Growth inhibition assay 2 days Growth inhibition of human U251 cells after 2 days by MTT assay, GI50 = 6.5 μM. 22541394
NCI-H1299 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay, IC50 = 6.74 μM. 29202397
AsPC1 Growth inhibition assay 48 hrs Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay, GI50 = 6.9 μM. 28395150
BGC823 Growth inhibition assay 72 hrs Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 7.1 μM. 23061376
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 7.881 μM. 26140961
DU145 Anticancer assay 72 hrs Anticancer activity against human DU145 cells after 72 hrs by MTT assay, GI = 7.9 μM. 21741834
Bel7402 Growth inhibition assay 72 hrs Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8 μM. 23061376
HeLa Function assay 20 mins Inhibition of HDAC in human HeLa cells using fluor de Lys as substrate incubated for 20 mins by microplate spectrofluorometric analysis, IC50 = 8.02 μM. 27060764
MGC803 Growth inhibition assay 72 hrs Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8.9 μM. 23061376
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, GI50 = 9.32 μM. 28629630
SMMC7721 Growth inhibition assay 72 hrs Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 11 μM. 23061376
HeLa Function assay 24 to 48 hrs Inhibition of HDAC in human HeLa cells using Boc-Lys(AC)-AMC as substrate after 24 to 48 hrs by spectrofluorometry, IC50 = 11.18 μM. 26996372
HeLa Function assay Inhibition of HDAC in HeLa cells, IC50 = 12.5892 μM. 17606370
SKHEP1 Growth inhibition assay 72 hrs Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 13 μM. 23061376
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50 = 18.37 μM. 28629630
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, GI50 = 19.09 μM. 28629630
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50 = 19.24 μM. 28629630
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, GI50 = 19.26 μM. 28629630
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 27.47 μM. 18701301
U251 Growth inhibition assay 2 days Growth inhibition of human U251 cells after 2 days by MTT assay, TGI = 40 μM. 22541394
HEK293 STF Function assay 24 hrs Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay. 19022675
U937 Function assay 5 uM 24 hrs Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis. 17447750
U937 Function assay Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay. 18381238
U937 Function assay Induction of histone H4 hyperacetylation in human U937 cells. 18381238
U937 Function assay Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay. 18381238
U937 Function assay Induction of granulocytic differentiation in human U937 cells. 18381238
HCT116 Function assay 10 uM 24 hrs Inhibition of HDAC1 in human HCT116 cells assessed as induction of hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. 20452226
NB4 Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis. 20491440
NB4 Function assay 5 uM 24 hrs Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis. 20491440
epithelial cells Function assay 1 uM 4, 6, and 8 days Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in short circuit currents at 1 uM for 4, 6, and 8 days relative to control. 19966789
Hela Function assay 0.6 uM 16 hrs Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy. 21696956
U937 Cell cycle arrest assay 5 uM 30 hrs Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry. 21215647
epithelial cells Function assay 5 uM Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM. 19966789
NB4 Function assay 5 uM 24 hrs Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis. 20491440
C127-LT Function assay 1 uM 24 hrs Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 1 uM after 24 hrs by fluorescence microscopy. 26996372
C127-LT Function assay 10 uM 24 hrs Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy. 26996372
HCT116 Function assay 10 uM 24 hrs Inhibition of HDAC2 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. 22321215
HCT116 Function assay 10 uM 24 hrs Inhibition of HDAC1 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. 22321215
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells. 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells. 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells. 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells. 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells. 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells. 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells. 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells. 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells. 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells. 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells. 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells. 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells. 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells. 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells. 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells. 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells. 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells). 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells. 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells. 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells. 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells. 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells. 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells. 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells. 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells. 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells. 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells. 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells. 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells. 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells. 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells. 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells. 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells. 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells. 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells. 29435139
HeLa Function assay 1 uM 6 hrs Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 1 uM after 6 hrs by Western blot analysis. 29787262
MV4-11 Apoptosis assay 5 uM 24 to 48 hrs Induction of apoptosis in human MV4-11 cells at 5 uM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry. 29738953
MV4-11 Function assay 200 nM 24 hrs Inhibition of class 1 HDAC in human MV4-11 cells assessed as hyperacetylation of histone H3 at 200 nM after 24 hrs by Western blot analysis. 29738953
HL60 Apoptosis assay 5 uM 48 hrs Induction of apoptosis in human HL60 cells assessed as decrease in procaspase-3 level at 5 uM after 48 hrs by Western blot analysis. 28415009
HL60 Apoptosis assay 5 uM 48 hrs Induction of apoptosis in human HL60 cells assessed as increase in cleaved caspase-3 level at 5 uM after 48 hrs by Western blot analysis. 28415009
HL60 Apoptosis assay 5 uM 48 hrs Induction of apoptosis in human HL60 cells assessed as increase in cleaved PARP level at 5 uM after 48 hrs by Western blot analysis. 28415009
MV4-11 Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. 29589441
HEL Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human HEL cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. 29589441
Jurkat Cell cycle arrest assay 5 uM 24 hrs Cell cycle arrest in human Jurkat cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. 29589441
MV4-11 Function assay 5 uM 24 hrs Inhibition of class 1 HDAC in human MV4-11 cells assessed as induction of histone hyperacetylation at 5 uM after 24 hrs by Western blot method. 29589441
LNCAP Function assay 10 uM 24 hrs Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation at 10 uM measured after 24 hrs relative to control. 27717544
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Biological Activity

Description Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Targets
HDAC1 [2]
(Cell-free assay)		 HDAC3 [2]
(Cell-free assay)
0.51 μM 1.7 μM
In vitro
In vitro MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. [1] MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. [2] MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP. [3]
Kinase Assay Standard HDAC Assays
Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.
Cell Research Cell lines A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells
Concentrations ~ 10 μM
Incubation Time 3 days
Method

Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration.
Experimental Result Images Methods Biomarkers Images PMID
Western blot AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3 Cleaved PARP Caspase 8 DR4 / DR5 TopoIIα / TopoIIβ 24203492
Immunofluorescence phalloidin / snail DR4 / DR5 H3K4Me3 / H3K9Me3 29855565
Growth inhibition assay Cell proliferation Cell viability 24203492
ELISA GCP-2 / MCP-2 / MIF 24241152
In Vivo
In vivo MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. [1] MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. [4] MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes. [5]
Animal Research Animal Models A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.
Dosages 12.3, 24.5 and 49 mg/kg
Administration Administered orally once daily 5 days per week for 4 weeks
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04708470 Recruiting Oropharyngeal Cancer|Neck Cancer|Human Papillomavirus|HPV|Anal Cancer|Cervical Cancer|Penile Cancer|Vulvar Cancer|Vaginal Cancer|Colon Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 5 2021 Phase 1|Phase 2
NCT03829930 Terminated Prostate Adenocarcinoma George Washington University May 1 2019 Phase 1
NCT03765229 Completed Melanoma UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals March 22 2019 Phase 2
NCT03473639 Completed Metastatic Breast Cancer|Breast Cancer University of Virginia|Syndax Pharmaceuticals January 29 2019 Phase 1

Chemical lnformation & Solubility

Molecular Weight 376.41 Formula

C21H20N4O3
CAS No. 209783-80-2 SDF Download Entinostat (MS-275) SDF
Smiles C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3
Storage (From the date of receipt)

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DMSO : 75 mg/mL ( (199.25 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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Frequently Asked Questions

Question 1:
I would like to use Entinostat（Catalog No.S1053） for animal study. What is your recommendation for the solvent? What is the role of PEG 300 in this case? Can I use DMSO only and dilute it with PBS or HBSS?

Answer:
2%DMSO/30%PEG/68%Water is recommended. PEG is an important polymer that helps with the solubility of hydrophobic drugs. If you use DMSO only and dilute it with PBS or HBSS, Entinostat will likely to precipitate out since it has very low solubility in water.

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