Home Cell Cycle CDK inhibitor BS-181 HCl For research use only.

BS-181 HCl

BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

BS-181 HCl Chemical Structure

BS-181 HCl Chemical Structure

CAS No. 1397219-81-6 

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Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Biological Activity

Description BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
Features Demonstrates higher inhibitory selectivity for CDK7 vs. other CDKs and kinases from other classes.
Targets
CDK7 [1]
(Cell-free assay)
21 nM
In vitro
In vitro BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 μM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines. [1]
Kinase Assay In vitro kinase inhibition.
Inhibition of CDK7 activity is measured by incubation of increasing amounts of BS-181 with purified recombinant CDK7/CycH/MAT1 complex, followed by measurement of free ATP remaining in the reaction using a luciferase assay, luciferase activity therefore providing a measure of inhibition of CDK7 activity for the determination of IC50.
Cell Research Cell lines MCF-7 cells
Concentrations Dissolved in DMSO, final concentration ~50 μM
Incubation Time 24 hours
Method MCF-7 cells are exposed to BS-181 for 24 hours. For the determination of cell cycle and apoptosis, cells are stained with propidium iodide or labeled with Annexin V-FITC, then labeled cells are acquired within 1 hour, by using the RXP cytomics software on a Beckman Coulter Elite ESP, and the data are analyzed using Flow Jo v7.2.5. For the assessment of CDKs, cells are lysed and analyzed by western blotting.
In Vivo
In vivo BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity. [1]
Animal Research Animal Models MCF-7 cells are established in female nu/nu-BALB/c athymic nude mice
Dosages 10 or 20 mg/kg
Administration Twice daily by i.p. injection

Chemical Information & Solubility

Molecular Weight 416.99 Formula

C22H32N6.HCl
CAS No. 1397219-81-6  SDF Download BS-181 HCl SDF
Smiles Cl.CC(C)C1=C2N=C(NCCCCCCN)C=C(NCC3=CC=CC=C3)[N]2N=C1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 83 mg/mL

Ethanol : 22 mg/mL


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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.

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