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BS-181

Catalog No. T1947   CAS 1092443-52-1
Synonyms: BS 181

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); <40-fold selective for CDK7 than CDK1/2/4/5/6/9.

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BS-181 Chemical Structure
BS-181, CAS 1092443-52-1
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10 mg Inquiry $ 150.00
50 mg Inquiry $ 498.00
1 mL * 10 mM (in DMSO) Inquiry $ 98.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9.
Targets&IC50 CDK7:21 nM
In vitro BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser795 and Ser821 with an apparent IC50 of 15 μM, similar to the IC50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis[1]. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC50) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner[2].
In vivo BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance[1]. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group[2].
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 viability is detected using Cell Counting Kit (CCK-8 kit) according to supplier's introductions. Briefly, BGC823 cells are seeded at 104?cells per well for 48 hours with or without BS-181. Then, the absorbance is detected at 450 nm (reference at 650 nm) in each well.
Synonyms BS 181
Molecular Weight 380.53
Formula C22H32N6
CAS No. 1092443-52-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM

TargetMolReferences and Literature

1. Cancer Res. 2009 Aug 1;69(15):6208-15. doi: 10.1158/0008-5472.CAN-09-0301. Epub 2009 Jul 28. 2. Wang BY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016 Mar 16;10:1181-9.

TargetMolCitations

1. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464.

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Keywords

BS-181 1092443-52-1 Apoptosis Cell Cycle/Checkpoint CDK Inhibitor Cyclin dependent kinase inhibit BS 181 BS181 inhibitor

 

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