Home PI3K/Akt/mTOR PP2A inhibitor LB-100 For research use only.

LB-100

LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

LB-100 Chemical Structure

LB-100 Chemical Structure

CAS: 1632032-53-1

Selleck's LB-100 has been cited by 43 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U251 cells Function assay 2 μM 3 hours and 6 hours treatment with 2 μM LB100 reduced PP2A activity to 61% of control cells after both three and six hours of LB100 exposure. 25939762
D283 cells Cell viability assay IC50=0.9 μM, using XTT assays 26799670
DAOY cells Cell viability assay IC50=2.9 μM, using XTT assays 26799670
D341 cells Cell viability assay IC50=1.9 μM, using XTT assays 26799670
CH-157 cells Function assay 2.5 μM 3 hours LB-100 significantly enhanced the proportion of cells in G2/M. 29199006
SKOV-3 Cytotoxicity assay 72 h IC50 = 10.1 ± 1.8 μM 25376608
OVCAR-8 Cytotoxicity assay 72 h IC50 = 5.5 ± 0.5 μM 25376608
PEO-4 Cytotoxicity assay 72 h IC50 = 5 ± 0.6 μM 25376608
PEO-6 Cytotoxicity assay 72 h IC50 = 5.1 ± 0.2 μM 25376608
PEO1-Brca2 Missense Cytotoxicity assay 72 h IC50 = 6.2 ± 1.5 μM 25376608
PEO1-Brca2 STOP Cytotoxicity assay 72 h IC50 = 6.2 ± 1.0 μM 25376608
Huh-7 PP2A activity assays 5 μmol/L 2 h reduced the activity of PP2A to about 70% 24867249
HepG2 PP2A activity assays 5 μmol/L 2 h reduced the activity of PP2A to about 70% 24867249
HL-7702 PP2A activity assays 5 μmol/L 2 h reduced the activity of PP2A to about 70% 24867249
Click to View More Cell Line Experimental Data

Biological Activity

Description LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Targets
PP2A [1]
In vitro
In vitro LB-100 inhibits the cell growth with IC50 of 2.3 μM (in BxPc-3) or 1.7 μM (in Panc-1 cell). In BxPc-3, Panc-1, and SW1990 cells, LB-100 reduces the PP2A activity by 30-50%. LB-100 increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. LB-100 increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.[1]
Kinase Assay PP2A activity assays
Cultured pancreatic cancer cells are treated with IC50 of LB-100 for each cell line or equal volume of vehicle for 2 hours, and PP2A activity assays are then performed using Ser/Thr phosphatase assay kit. Cells are lysed with an ultrasonic cell disruptor, and the PP2A concentration is measured using a Ser/Thr phosphatase assay kit according to the instructions. Assays for each cell line are performed in triplicate.
Cell Research Cell lines BxPc-3, and Panc-1 cell lines
Concentrations ~ 10 μM
Incubation Time 48 h
Method

Cytotoxicity is conducted by using a Cell Counting Kit-8. Cells are seeded in 96-well plates with a density of 3000 cells per well and are assessed after treatments following the CCK-8 protocol. Relative cytotoxicity is expressed as a percentage of specific controls.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Cyclin D1 / c-myc / mcl-1 / Hsp90 29199006
Growth inhibition assay Cell division Cell viability 29844427
In Vivo
In vivo In a mouse pancreatic cancer xenograft model, LB-100 (2 mg/kg, i.p.) enhances chemotherapy of doxorubicin. LB-100 causes higher density of microvessel in tumors and rapid blood flow at the surface of tumors. [1]
Animal Research Animal Models BALB/c nude mice bearing Panc-1 xenograft
Dosages 2 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06012734 Not yet recruiting Metastatic Microsatellite-stable Colorectal Cancer The Netherlands Cancer Institute December 2023 Phase 1
NCT03886662 Unknown status Myelodysplastic Syndromes Lixte Biotechnology Holdings Inc. April 2019 Phase 1|Phase 2
NCT03027388 Completed Astrocytoma Grades II III and IV|Glioblastoma Multiforme|Giant Cell Glioblastoma|Glioma|Oligodendrogliomas National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 9 2019 Phase 2
NCT01837667 Completed Tumors|Neoplasms|Cancer Lixte Biotechnology Holdings Inc. February 2013 Phase 1

Chemical lnformation & Solubility

Molecular Weight 268.31 Formula

C13H20N2O4
CAS No. 1632032-53-1 SDF Download LB-100 SDF
Smiles CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3
Storage (From the date of receipt)

In vitro
Batch:

Water : 54 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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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

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