BS-181 HCl

For research use only.

Catalog No.S1572

14 publications

BS-181 HCl Chemical Structure

CAS No. 1397219-81-6 

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  
10mM (1mL in DMSO) EUR 412 In stock
EUR 314 In stock
EUR 953 In stock
EUR 2132 In stock
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Selleck's BS-181 HCl has been cited by 14 publications

4 Customer Reviews

  • 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.

  • B, SK-OV-3, KB, and KB/VCR cells were pretreated with a CDK7-specific inhibitor and then assayed for RPB1.

    Mol Cancer Ther, 2016, 15(7):1495-503. BS-181 HCl purchased from Selleck.

  • 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.

  • (a) COCs were collected from large antral follicles and treated with CDK inhibitors for 22 h. The COCs were then released from the inhibitors, cultured under normal conditions, denuded, and subjected to immunostaining with an anti-lamin A/C antibody (green) to detect the germinal vesicle (GV) situation. DNA was counterstained with DAPI and is pseudo-colored red for better visualization.

    Reprod Biol, 2017, 1.446. 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.
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]


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
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
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


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID