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BS-181

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.
Catalog No. T1947Cas No. 1092443-52-1
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BS-181

Catalog No. T1947Alias BS 181Cas No. 1092443-52-1

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$88Backorder
10 mg$150Backorder
50 mg$498Backorder
1 mL x 10 mM (in DMSO)$98Backorder
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Product Introduction

Bioactivity
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.
AliasBS 181
Chemical Properties
Molecular Weight380.53
FormulaC22H32N6
Cas No.1092443-52-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 10 mM
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6279 mL13.1396 mL26.2791 mL131.3957 mL
5 mM0.5256 mL2.6279 mL5.2558 mL26.2791 mL
10 mM0.2628 mL1.3140 mL2.6279 mL13.1396 mL

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