BS-181 HCl

Catalog No.S1572

BS-181 HCl Chemical Structure

Molecular Weight(MW): 416.99

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.

Size Price Stock Quantity  
In DMSO USD 420 In stock
USD 320 In stock
USD 970 In stock
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2 Customer Reviews

  • Relative sensitivity of UKF-NB-3 and UKF-NB-3rSNS-032300nM to the CDK2, 7, and 9 inhibitor seliciclib, the CDK7 inhibitor LDC000067, the CDK9 inhibitor BS-181, or the CDK 1,2,4,6,7, and 9 inhibitor alvocidib.

    Oncotarget, 2016, 7(36):58051-58064. BS-181 HCl purchased from Selleck.

    Dose-response inhibition of purified human recombinant cyclin-dependent kinase CDK7/cyclin H by inhibitor BS-181 (left panel). Immunoblotting of RNA polymerase II and its phosphorylated form (at Ser5), physiological substrate of CDK7, in MCF-7 cells treated with different doses of inhibitor BS-181 for 24 h (right panel).

    Dr. Vladimir Krystof of Palacky University. BS-181 HCl purchased from Selleck.

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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

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]

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]

Protocol

Kinase Assay:[1]
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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:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: MCF-7 cells are established in female nu/nu-BALB/c athymic nude mice
  • Formulation: Prepared in the vehicle of 10% DMSO / 50 mM HCl / 5% Tween 20 / 85% saline.
  • Dosages: 10 or 20 mg/kg
  • Administration: Twice daily by i.p. injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.04 mM)
Ethanol 22 mg/mL warmed (52.75 mM)
Water 3 mg/mL (7.19 mM)
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 416.99
Formula

C22H32N6.HCl

CAS No. 1397219-81-6 
Storage powder
Synonyms N/A

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID