BS-181 dihydrochloride
Based on 7 publication(s) in Google Scholar
BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.
For research use only. We do not sell to patients.
- CAS No.: 1883548-83-1
- Formula: C22H34Cl2N6
- Molecular Weight:453.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BS-181 dihydrochloride
More- Theranostics. 2017 Apr 20;7(7):1914-1927. [Abstract]
- Int J Biol Macromol. 2025 Mar:294:139117. [Abstract]
- Cell Rep. 2017 Dec 5;21(10):2796-2812. [Abstract]
- Virulence. 2026 Dec;17(1):2629100. [Abstract]
- Biochem Biophys Res Commun. 2019 Jun 11;513(4):967-973. [Abstract]
- Res Sq. 2025 Dec 18.
- Universidade de Lisboa. 2021 Dec 21.
Customer Validation & Images
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WB
Biological Activity
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CDK7 21 nM (IC50) |
CDK2 880 nM (IC50) |
CDK5 3000 nM (IC50) |
CDK9 4200 nM (IC50) |
BS-181 dihydrochloride (0-40 μM; 72 hours) inhibits cancer cells growth, it is against Breast cancer cell lines growth with IC50 values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC50 values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC50 values ranging from 11.5 μM to 37.3 μM, respectively[1].BS-181 dihydrochloride (0-50 μM; 4 hours) shows inhibition of phosphorylation of the RNA polymerase II C-terminal domain (CTD) at serine 5 (P-Ser5). It down-regulates CDK4 and cyclin D1 expression while does not effect other CDKs and cyclins[1].BS-181 dihydrochloride (0-50 μM; 24 hours) shows an increase in cells in G1, accompanied by a reduction in cell numbers in S and G2/M at low concentrations. At higher concentrations, however, cells accumulates in the sub-G1, indicative of apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Breast cancer cell line: MCF-7, MDA-MB-231, T47D, ZR-75-1, etcColorectal cancer cell line: COLO-205, HCT-116, HCT-116 (p53-/-)Lung cancer cell line: A549, NCI-460Osteosarcoma cancer cell line: U2OS, SaOS2Prostate cancer cell line: PC3, LNCaP
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Concentration:0-40 μM
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Incubation Time:72 hours
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Result:Had anti-proliferative activities against a panel of cell lines, including breast, lung, prostate and colorectal cancer.
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Cell Line:Breast cancer cell line: MCF-7 cells
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Concentration:0 μM; 25 μM; 50 μM
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Incubation Time:4 hours
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Result:Inhibited phosphorylation of CDK7 substrates.
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Cell Line:Breast cancer cell line: MCF-7 cells
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Concentration:0 μM; 25 μM; 50 μM
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Incubation Time:24 hours
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Result:Led cells to G1 arrest and apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:7-week old female nu/nu-BALB/c athymic nude mice with MCF-7 cells[1]
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Dosage:5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg
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Administration:Intraperitoneal injection; twice daily or once total daily; 14 days
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Result:Inhibited tumor growth significantly.
Chemical Information
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CAS No. 1883548-83-1
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Molecular Weight 453.45
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Formula C22H34Cl2N6
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SMILES
CC(C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCCCCCCN)C.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Theranostics
Triptolide Inhibits the AR Signaling Pathway to Suppress the Proliferation of Enzalutamide Resistant Prostate Cancer Cells. [Abstract]2017 Apr 20;7(7):1914-1927. PMID: 28638477
BS-181 dihydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2017 Apr 20;7(7):1914-1927. [Abstract]
Effect of TPL on the levels of pAR S515 and related proteins in PCa cells. LNCaP and C4-2/AR-V7 cells are pretreated with TPL or BS-181 for 1 h, and then incubated with R1881 for 4 h.
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Int J Biol Macromol
CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609. [Abstract]2025 Mar:294:139117. PMID: 39733900 -
Cell Rep
Melanoma Therapeutic Strategies that Select against Resistance by Exploiting MYC-Driven Evolutionary Convergence. [Abstract]2017 Dec 5;21(10):2796-2812. PMID: 29212027 -
Virulence
The cyclin dependent kinase (CDK)7 inhibitor BS-181 inhibits pathogenic Cryptococcus species, causing G2/M arrest and a splicing defect. [Abstract]2026 Dec;17(1):2629100. PMID: 41701636 -
Biochem Biophys Res Commun
2019 Jun 11;513(4):967-973. PMID: 31005255 -
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Purity & Documentation
References
[1]. Ali S et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009 Aug 1;69(15):6208-15. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BS-181 dihydrochloride Related Classifications
HY-110368 Related Classifications
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