Home TGF-beta/Smad Antineoplastic and Immunosuppressive Antibiotics inhibitor - PKC inhibitor - ADC Cytotoxin - PKA inhibitor - S6 Kinase inhibitor - CaMK inhibitor - PKG inhibitor Staurosporine (STS) For research use only.

Staurosporine (STS)

Synonyms: AM-2282，Antibiotic AM-2282

Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

Staurosporine (STS) Chemical Structure

Staurosporine (STS) Chemical Structure

CAS: 62996-74-1

Selleck's Staurosporine (STS) has been cited by 153 publications

Purity & Quality Control

Batch: Purity: 99.61%
99.61

Products often used together with Staurosporine (STS)

5-FU (5-Fluorouracil)

Staurosporine and 5-FU (5-Fluorouracil) combination exhibits a 2-fold higher induction of apoptosis in Lovo B2 cells.

Sigmond J, et al. Nucleosides Nucleotides Nucleic Acids. 2004 Oct;23(8-9):1503-6.

Oxaliplatin

Staurosporine and Oxaliplatin use results in the accumulation of DAPI+ cells in human non-small cell lung carcinoma A549 cells.

Sauvat A, et al. Oncotarget. 2015 Apr 20;6(11):9467-75.

Prostaglandin E2 (PGE2)

Staurosporine and Prostaglandin E2 treatment enhances the transduction of human CD34+ and increases the transduction of human short-term NSG repopulating cells.

Lewis G, et al. Mol Ther Methods Clin Dev. 2018 Apr 5;9:313-322.

Retinoic acid (Tretinoin)

Staurosporine and Retinoic acid combination induces granulocytic differentiation accompanied by inhibition of proliferation in NB4-R1/NB4-R2 cells.

Ge DZ, et al. Sci Rep. 2014 Apr 28;4:4821.

Z-VAD-FMK

Z-VAD-FMK inhibits staurosporine-induced cell death in SJG2/MT330 cells.

Wang R, et al. Biochem Biophys Res Commun. 2016 Sep 9;478(1):128-134.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human colon carcinoma cell line HCT116 Function assay Concentration required for growth inhibition of human colon carcinoma cell line HCT116, IC50=6 nM. 15537345
human PBMC Function assay 24 h Suppression of IL2 production in human PBMC after 24 hrs by ELISA, IC50=16 nM. 18585046
endothelial cells Function assay Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50 = 7.5 μM. 8709095
Sf9 insect cells Function assay Inhibition of protein kinase C(1:1mixture of PKC alpha & beta) expressed in Sf9 insect cells, IC50 = 0.02 μM. 9873605
LoVo cells Antiproliferative activity assay Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay, IC50 = 0.001 μM. 11591505
umbilical vein endothelial cells Antiproliferative activity assay Antiproliferative activity against human umbilical vein endothelial cells (HUVECs) using MTT assay, IC50 = 0.004 μM. 11591505
ST-486 cells Antiproliferative activity assay Antiproliferative activity against burkit lymphoma cell line (ST-486 cells) using MTT assay, IC50 = 0.007 μM. 11591505
DLD-1 cells Antiproliferative activity assay Antiproliferative activity against human colon cancer cell line (DLD-1 cells) using MTT assay, IC50 = 0.009 μM. 11591505
HEK293 cells Function assay Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA, IC50 = 0.077 μM. 12941331
P19 cells Function assay Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM. 15771419
P19 cells Function assay Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM. 15771419
P19 cells Function assay Inhibition of Protein Kinase A in P19 cells, IC50 = 0.004 μM. 15771419
P19 cells Function assay Inhibition of Calcium/calmodulin-dependent protein kinase type II in P19 cells, IC50 = 0.006 μM. 15771419
P19 cells Function assay Inhibition of Cyclin-dependent kinase 1 in P19 cells, IC50 = 0.008 μM. 15771419
P19 cells Function assay Inhibition of Vascular endothelial growth factor receptor in P19 cells, IC50 = 0.014 μM. 15771419
HEK293 cells Function assay Inhibition of IL-8 release by HEK293 cells expressing PKC-beta2, IC50 = 0.077 μM. 15771419
P19 cells Function assay Inhibition of Insulin receptor kinase in P19 cells, IC50 = 0.2 μM. 15771419
P19 cells Function assay Inhibition of Casein kinase 1 in P19 cells, IC50 = 1.4 μM. 15771419
FL5.12-Akt1 cells Antiproliferative activity assay Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50 = 0.29 μM. 16403626
MiaPaCa-2 cells Antiproliferative activity assay Antiproliferative activity against MiaPaCa-2 cells by MTT assay, IC50 = 0.37 μM. 16403626
FL5.12-Akt1 cells Function assay Activity against GSK3 in FL5.12-Akt1 cells, EC50 = 0.46 μM. 16403626
MiaPaCa-2 cells Antiproliferative activity assay Antiproliferative activity against human MiaPaCa-2 cells, IC50 = 0.37 μM. 16413780
FL5.12-Akt1 cells Function assay Activity against GSK3 phosphorylation in FL5.12-Akt1 cells, EC50 = 0.46 μM. 16413780
Sf21 cells Function assay Inhibition of JAK3 expressed in Sf21 cells, IC50 = 0.006 μM. 17088059
U937 cells Cytotoxicity assay Cytotoxicity against human U937 cells, IC50 = 2 μM. 17088067
Sf9 cells Function assay 1 min Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 1 umol/L ATP, IC50 = 0.005 μM. 17315853
Sf9 cells Function assay 20 mins Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 1 umol/L ATP, IC50 = 0.015 μM. 17315853
Sf9 cells Function assay 1 min Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 10 umol/L ATP, IC50 = 0.036 μM. 17315853
Sf9 cells Function assay 20 mins Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 10 umol/L ATP, IC50 = 0.083 μM. 17315853
Sf9 cells Function assay 1 min Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 100 umol/L ATP, IC50 = 0.27 μM. 17315853
Sf9 cells Function assay 20 mins Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 100 umol/L ATP, IC50 = 0.51 μM. 17315853
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0024 μM. 18484775
MDA-MB-231 cells Cytotoxicity assay 72 h Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0071 μM. 18484775
HT29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0109 μM. 18484775
MCF7 cells Function assay Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, Ki = 0.005 μM. 18656369
MCF7 cells Function assay Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, IC50 = 2 μM. 18656369
Sf9 cells Function assay Inhibition of human Syk expressed in Sf9 cells, IC50 = 0.003 μM. 18823784
Sf9 cells Function assay Inhibition of human ZAP70 expressed in Sf9 cells, IC50 = 0.053 μM. 18823784
insect cells Function assay Inhibition of human recombinant Pim1 expressed in insect cells by HTRF, IC50 = 0.01 μM. 19179076
HT-29 cells Apoptosis assay 2 h Induction of apoptosis in human HT-29 cells assessed as change in mitochondrial transmembrane potential after 2 hrs by JC1 staining based fluorescence assay, ED50 = 0.0026 μM. 19422206
insect Sf21 cells Function assay Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation, IC50 = 0.006 μM. 19427203
Jurkat cells Antiproliferative activity assay Antiproliferative activity against JAK3 expressing IL2-stimulated human Jurkat cells, IC50 = 0.071 μM. 19427203
Jurkat cells Antiproliferative activity assay Antiproliferative activity against JAK3 expressing human resting Jurkat cells, IC50 = 0.311 μM. 19427203
HUE cells Function assay 90 mins Inhibition of VEGFR2 in HUE cells assessed as inhibition of VEGF-induced autophosphorylation treated for 90 mins before VEGF challenge by ELISA, IC50 = 0.07 μM. 20170163
Sf9 cells Function assay 60 mins Inhibition of human recombinant GST-fused NIK expressed in Sf9 cells after 60 mins by radiometric protein kinase assay, IC50 = 2.3 μM. 20580552
Sf21 cells Function assay 30 uM Inhibition of human CHK2 kinase expressed in insect Sf21 cells using phospho-CREBtide as substrate at 30 uM, IC50 = 0.027 μM. 21334796
Sf21 cells Function assay 30 uM Inhibition of human recombinant IKK-alpha expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.039 μM. 21334796
Sf21 cells Function assay 30 uM Inhibition of human recombinant IKK-beta expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.49 μM. 21334796
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM. 21388191
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM. 21388191
HT-29 cells Function assay 2 h Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay, IC50 = 0.002 μM. 21428375
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM. 21488655
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM. 21488655
HT-29 cells Function assay Inhibition of mitochondrial membrane potential in human HT-29 cells using JC1 dye staining by fluorescence plate reader assay, IC50 = 0.0025 μM. 21513293
SF268 cells Cytotoxicity assay 48 h Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50 = 0.044 μM. 21513294
CHOK1 cells Cytotoxicity assay 48 h Cytotoxicity against human CHOK1 cells after 48 hrs by SRB assay, GI50 = 0.13 μM. 21513294
H460 cells Cytotoxicity assay 48 h Cytotoxicity against human H460 cells after 48 hrs by SRB assay, GI50 = 3.6 μM. 21513294
HT-29 cells Cytotoxicity assay 48 h Cytotoxicity against human HT-29 cells after 48 hrs by SRB assay, GI50 = 3.6 μM. 21513294
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 11 μM. 21513294
SW1116 cells Function assay 24 h Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.32 μM. 21962523
HT-29 cells Apoptosis assay 2 h Induction of apoptosis in human HT-29 cells assessed reduction of mitochondrial membrane potential after 2 hrs by using JC1 staining by fluorescence cell-based assay, ED50 = 0.0026 μM. 21973101
LoVo cells Antiproliferative activity assay 48 to 72 h Antiproliferative activity against human LoVo cells after 48 to 72 hrs by MTT assay, IC50 = 0.001 μM. 22182929
ST486 cells Antiproliferative activity assay 48 to 72 h Antiproliferative activity against human ST486 cells after 48 to 72 hrs by MTT assay, IC50 = 0.007 μM. 22182929
DLD1 cells Antiproliferative activity assay 48 to 72 h Antiproliferative activity against human DLD1 cells after 48 to 72 hrs by MTT assay, IC50 = 0.009 μM. 22182929
B16F10 cells Antiproliferative activity assay 48 h Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 2.82 μM. 22503364
MCF7 cells Antiproliferative activity assay 48 h Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 3.07 μM. 22503364
A431 cells Cytotoxicity assay 24 h Cytotoxicity against human A431 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.07 μM. 22541051
MCF7 cells Cytotoxicity assay 24 h Cytotoxicity against human MCF7 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.18 μM. 22541051
BJ cells Cytotoxicity assay 72 h Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay, IC50 = 0.002 μM. 22921081
CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay, IC50 = 0.023 μM. 22921081
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay, IC50 = 0.064 μM. 22921081
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay, IC50 = 0.175 μM. 22921081
HepG2 cells Function assay 24 h Inhibition of telomerase in human HepG2 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.14 μM. 23018096
SW1116 cells Antiproliferative activity assay 48 h Antiproliferative activity against human SW1116 cells after 48 hrs by MTT method, IC50 = 4.95 μM. 23018096
HepG2 cells Antiproliferative activity assay 48 h Antiproliferative activity against human HepG2 cells after 48 hrs by MTT method, IC50 = 6.73 μM. 23018096
BGC823 cells Antiproliferative activity assay 48 h Antiproliferative activity against human BGC823 cells after 48 hrs by MTT method, IC50 = 6.83 μM. 23018096
HeLa cells Antiproliferative activity assay 48 h Antiproliferative activity against human HeLa cells after 48 hrs by MTT method, IC50 = 9.12 μM. 23018096
HCT116 cells Function assay Inhibition of TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells by beta-lactamase reporter gene assay, IC50 = 0.039 μM. 23232060
HepG2 cells Function assay 48 h Inhibition of telomerase in human HepG2 cells after 48 hrs by TRAP-PCR-ELISA, IC50 = 8.3 μM. 23279864
SW1116 cells Function assay 24 h Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.18 μM. 24286761
KE-97 cells Cytotoxicity assay 72 h Cytotoxicity against human KE-97 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.13 μM. 24328283
Jurkat cells Cytotoxicity assay 72 h Cytotoxicity against human Jurkat cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.14 μM. 24328283
HuH7 cells Cytotoxicity assay 72 h Cytotoxicity against human HuH7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.23 μM. 24328283
BGC823 cells Cytotoxicity assay 72 h Cytotoxicity against human BGC823 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.38 μM. 24328283
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.52 μM. 24328283
NIH/3T3 cells Cytotoxicity assay 96 h Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
A2780 cells Cytotoxicity assay 96 h Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
HT-29 cells Cytotoxicity assay 96 h Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
8505C cells Cytotoxicity assay 96 h Cytotoxicity against human 8505C cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
518A2 cells Cytotoxicity assay 96 h Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50 = 0.2 μM. 24361521
MCF7 cells Cytotoxicity assay 96 h Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 0.4 μM. 24361521
A549 cells Cytotoxicity assay 96 h Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50 = 0.6 μM. 24361521
V79 MZ cells Function assay Inhibition of human aldosterone synthase expressed in V79 MZ cells assessed as inhibition of aldosterone synthesis, IC50 = 0.011 μM. 24422519
HEK293 cells Cytotoxicity assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay, IC50 = 0.056 μM. 24763262
HeLa cells Antiproliferative activity assay 24 to 48 h Antiproliferative activity against human HeLa cells after 24 to 48 hrs by CCK-8 assay, IC50 = 2.72 μM. 24792811
A549 cells Antiproliferative activity assay 24 to 48 h Antiproliferative activity against human A549 cells after 24 to 48 hrs by CCK-8 assay, IC50 = 3.05 μM. 24792811
HepG2 cells Cytotoxicity assay Cytotoxicity against human HepG2 cells, EC50 = 2 μM. 25316317
Raji cells Cytotoxicity assay Cytotoxicity against human Raji cells, EC50 = 2 μM. 25316317
BJ cells Cytotoxicity assay Cytotoxicity against human BJ cells, EC50 = 2 μM. 25316317
HEK293 cells Cytotoxicity assay Cytotoxicity against HEK293 cells, EC50 = 2 μM. 25316317
A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.02 μM. 25825934
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.025 μM. 25825934
PC3 cells Cytotoxicity assay 48 h Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 0.031 μM. 25825934
MGC-803 cells Function assay 24 h Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.97 μM. 26900656
Sf9 insect cells Function assay 10 mins Inhibition of N-terminal GST tagged recombinant full-length human CHK1 expressed in baculovirus Sf9 insect cells after 10 mins by luminescent ADP-Glo assay, IC50 = 0.0012 μM. 27089211
Sf21 cells Function assay 60 mins Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method, IC50 = 0.002 μM. 27137359
Neuro2a cells Cytotoxicity assay 72 h Cytotoxicity against mouse Neuro2a cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0113 μM. 28152427
MDA-MB-231 cells Function assay 16 h Inhibition of retinoblastoma protein phosphorylation in human MDA-MB-231 cells after 16 hrs by Hoechst 33342 staining based fluorescence assay, IC50 = 0.066 μM. 28431342
Sf9 insect cells Function assay 20 mins Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50 = 0.00029 μM. 28482151
HEK293 cells Cytotoxicity assay 72 h Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay, CC50 = 0.00354 μM. 28624701
BT549 cells Cytotoxicity assay 24 h Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay, IC50 = 0.08 μM. 28705432
MDA-MB-468 cells Cytotoxicity assay 24 h Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay, IC50 = 0.15 μM. 28705432
MDA-MB-231 cells Cytotoxicity assay 24 h Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay, IC50 = 0.24 μM. 28705432
Vero cells Cytotoxicity assay 2 days Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 2 days by cell-titer-glo luminescent assay, TC50 = 0.0024 μM. 28763645
L929 cells Antiproliferative activity assay 5 days Antiproliferative activity against mouse L929 cells after 5 days by WST-1 assay, IC50 = 0.2 μM. 28956915
KB-3-1 cells Antiproliferative activity assay 5 days Antiproliferative activity against human KB-3-1 cells after 5 days by WST-1 assay, IC50 = 0.2 μM. 28956915
MCF7 cells Antiproliferative activity assay 5 days Antiproliferative activity against human MCF7 cells after 5 days by WST-1 assay, IC50 = 1.8 μM. 28956915
FS4-LTM cells Antiproliferative activity assay 24 h Antiproliferative activity against human FS4-LTM cells after 24 hrs by WST-1 assay, IC50 = 2.8 μM. 28956915
Vero cells Cytotoxicity assay 2 days Cytotoxicity against African green monkey Vero cells after 2 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.0024 μM. 28993106
HepG2 cells Cytotoxicity assay 100 uM 3 days Cytotoxicity against human HepG2 cells at 100 uM after 3 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.018 μM. 28993106
NIH/3T3 cells Cytotoxicity assay 96 h Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, EC50 = 0.008 μM. 29197730
518A2 cells Cytotoxicity assay 96 h Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, EC50 = 0.03 μM. 29197730
A549 cells Cytotoxicity assay 96 h Cytotoxicity against human A549 cells after 96 hrs by SRB assay, EC50 = 0.04 μM. 29197730
MCF7 cells Cytotoxicity assay 96 h Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, EC50 = 0.1 μM. 29197730
A2780 cells Cytotoxicity assay 96 h Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, EC50 = 0.12 μM. 29197730
HT-29 cells Cytotoxicity assay 96 h Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, EC50 = 0.15 μM. 29197730
PC3 cells Cytotoxicity assay Cytotoxicity against human PC3 cells by sulforhodamine B assay, IC50 = 0.017 μM. 29389122
HCT116 cells Cytotoxicity assay Cytotoxicity against human HCT116 cells by sulforhodamine B assay, IC50 = 0.055 μM. 29389122
insect cells Function assay 30 mins Inhibition of recombinant human PDGFRbeta expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 30 mins by LANCE method, IC50 = 0.00076 μM. 29549836
Sf9 insect cells Function assay 60 mins Inhibition of recombinant human KDR expressed in Sf9 insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.0021 μM. 29549836
insect cells Function assay 10 mins Inhibition of recombinant human Src expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 10 mins by LANCE method, IC50 = 0.005 μM. 29549836
insect cells Function assay 15 mins Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM. 29549836
insect cells Function assay 15 mins Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM. 29549836
Sf9 insect cells Function assay 15 mins Inhibition of recombinant human Flt1 expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 15 mins by LANCE method, IC50 = 0.035 μM. 29549836
Sf21 insect cells Function assay 15 mins Inhibition of recombinant human Aurora-A expressed in Sf21 insect cells using Ulight-RRRSLLE as substrate after 15 mins by LANCE method, IC50 = 0.039 μM. 29549836
insect cells Function assay 60 mins Inhibition of recombinant human AKT1 expressed in insect cells using CREBtide as substrate after 60 mins by LANCE method, IC50 = 0.056 μM. 29549836
Sf9 insect cells Function assay 60 mins Inhibition of recombinant human FAK expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.062 μM. 29549836
insect cells Function assay 60 mins Inhibition of recombinant human ABL expressed in insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.29 μM. 29549836
insect cells Function assay 60 mins Inhibition of recombinant human c-MET expressed in insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.31 μM. 29549836
PC3 cells Cytotoxicity assay 72 h Cytotoxicity against human PC3 cells after 72 hrs by SRB assay, IC50 = 0.039 μM. 29558119
Sf9 cells Function assay 45 mins Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.047 μM. 29902719
Sf9 cells Function assay 45 mins Inhibition of recombinant human N-terminal GST-tagged HER2 (679 to 1255 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.0608 μM. 29902719
HT-29 cells Function assay 3 h Inhibition of mitochondrial membrane potential in human HT-29 cells after 3 hrs by JC-1 staining based fluorescence assay, IC50 = 0.02 μM. 30057155
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM. 30067358
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM. 30067358
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM. 30067358
Sf9 cells Function assay Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM. 30067358
HCT116 cells Cytotoxicity assay 48 h Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.03 μM. 30106291
Huh7.5 cells Cytotoxicity assay 48 h Cytotoxicity against human Huh7.5 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.6 μM. 30106291
K562 cells Cytotoxicity assay 48 h Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM. 30106291
LO2 cells Cytotoxicity assay 48 h Cytotoxicity against human LO2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 9.5 μM. 30106291
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Biological Activity

Description Staurosporine (STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Targets
PKCα [1]
(Cell-free assay)		 c-Fgr [2]
(Cell-free assay)		 phosphorylase kinase [2]
(Cell-free assay)		 PKCη [1]
(Cell-free assay)		 PKCγ [1]
(Cell-free assay)		 Click to View More Targets
2 nM 2 nM 3 nM 4 nM 5 nM
In vitro
In vitro Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively. [2] Staurosporine (1 μM) induces >90% apoptosis in PC12 cells. Consistently, Staurosporine treatment induces a rapid and prolonged elevation of intracellular free calcium levels [Ca2+]i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. [3] The apoptosis of MCF7 cells induced by Staurosporine can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Staurosporine treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. [6] In addition to activating the classical mitochondrial apoptosis pathway, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1. [7]
Kinase Assay Enzyme assay and binding assay
Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine.
Cell Research Cell lines PC12
Concentrations Dissolved in DMSO, final concentration 1 μM
Incubation Time ~32 hours
Method

Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Akt / Akt / PARP /Cleaved PARP FAK / RIP Ambra1 24174874
Growth inhibition assay Cell viability 25215174
Immunofluorescence Tubulin / Actin Phalloidin / Type II collagen Pyk2 Annexin cleaved-caspase 3 FAK 4.47 25215174
In Vivo
In vivo In the gerbil and rat ischemia models, Staurosporine pretreatment (0.1-10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CAl pyramidal cell death after ischemia. [8]
Animal Research Animal Models Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
Dosages ~10 ng
Administration Stereotaxically administered into the bilateral CAl subfield of the hippocampus
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05209347 Withdrawn Ankle Fractures|Post-traumatic Osteoarthritis|Osteoarthritis Ankle University of Iowa December 2024 Not Applicable
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Chemical lnformation & Solubility

Molecular Weight 466.53 Formula

C28H26N4O3
CAS No. 62996-74-1 SDF Download Staurosporine (STS) SDF
Smiles CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (98.6 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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.

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