1. Cell Cycle/DNA Damage
  2. CDK
  3. BS-181 dihydrochloride

BS-181 dihydrochloride 

Cat. No.: HY-110368
Handling Instructions

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.

BS-181 dihydrochloride Chemical Structure

BS-181 dihydrochloride Chemical Structure

CAS No. : 1883548-83-1

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Top Publications Citing Use of Products

    BS-181 dihydrochloride purchased from MCE. Usage Cited in: Theranostics. 2017 Apr 20;7(7):1914-1927.

    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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    Description

    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[1][2].

    IC50 & Target[1]

    CDK7

    21 nM (IC50)

    CDK2

    880 nM (IC50)

    CDK5

    3000 nM (IC50)

    CDK9

    4200 nM (IC50)

    In Vitro

    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].

    Cell Proliferation Assay[1]

    Cell Line: Breast cancer cell line: MCF-7, MDA-MB-231, T47D, ZR-75-1, etc
    Colorectal cancer cell line: COLO-205, HCT-116, HCT-116 (p53-/-)
    Lung cancer cell line: A549, NCI-460
    Osteosarcoma cancer cell line: U2OS, SaOS2
    Prostate cancer cell line: PC3, LNCaP
    Concentration: 0-40 μM
    Incubation Time: 72 hours
    Result: Had anti-proliferative activities against a panel of cell lines, including breast, lung, prostate and colorectal cancer.

    Western Blot Analysis[1]

    Cell Line: Breast cancer cell line: MCF-7 cells
    Concentration: 0 μM; 25 μM; 50 μM
    Incubation Time: 4 hours
    Result: Inhibited phosphorylation of CDK7 substrates.

    Apoptosis Analysis[1]

    Cell Line: Breast cancer cell line: MCF-7 cells
    Concentration: 0 μM; 25 μM; 50 μM
    Incubation Time: 24 hours
    Result: Led cells to G1 arrest and apoptosis.
    In Vivo

    BS-181 dihydrochloride (intraperitoneal injection; 10 mg/kg, 20 mg/kg; single dose) is well tolerated in mice without apparent weight altering[1].
    BS-181 dihydrochloride (intraperitoneal injection; 5 mg/kg or 10 mg/kg twice daily; total daily doses of 10 mg/kg or 20 mg/kg; 14 days) inhibitstumor growth in a dose-dependent manner. Tumor growth exhibits 25% and 50% reduction compared with the control group, for 10 mg/kg/day and 20 mg/kg/day, respectively[1].

    Animal Model: 7-week old female nu/nu-BALB/c athymic nude mice with MCF-7 cells[1]
    Dosage: 5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg
    Administration: Intraperitoneal injection; twice daily or once total daily; 14 days
    Result: Inhibited tumor growth significantly.
    Molecular Weight

    453.45

    Formula

    C₂₂H₃₄Cl₂N₆

    CAS No.

    1883548-83-1

    SMILES

    CC(C1=C2N=C(C=C(N2N=C1)NCC3=CC=CC=C3)NCCCCCCN)C.Cl.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    BS-181BS181BS 181CDKCyclin dependent kinaseMCF-7MDA-MB-231T47DZR-75-1cancerCAKlungosteosarcomaprostatecancer therapytumorInhibitorinhibitorinhibit

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    Product Name:
    BS-181 dihydrochloride
    Cat. No.:
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