2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. BS-181

BS-181 

Cat. No.: HY-13266
COA Handling Instructions

BS-181 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, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (BS-181 hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

BS-181 Chemical Structure

BS-181 Chemical Structure

CAS No. : 1092443-52-1

Size Price Stock
Solution
10 mM * 1 mL in DMSO USD 121 Ask For Quote & Lead Time
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 121 Ask For Quote & Lead Time
Solid
5 mg USD 110 Ask For Quote & Lead Time
10 mg USD 180 Ask For Quote & Lead Time
50 mg USD 610 Ask For Quote & Lead Time

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BS-181 Related Antibodies

Top Publications Citing Use of Products

    BS-181 purchased from MCE. 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.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BS-181 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, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy[1][2].

    IC50 & Target[1]

    CDK7/CycH/MAT1

    0.021 μM (IC50)

    CDK2/Cyc E

    0.88 μM (IC50)

    CDK5/p35NCK

    3 μM (IC50)

    CDK9/cycT

    4.2 μM (IC50)

    CDK1/cycB

    8.1 μM (IC50)

    CDK4/Cyc D1

    33 μM (IC50)

    CDK6/cycD1

    47 μM (IC50)

    In Vitro

    BS-181 (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 (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 (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    BS-181 Related Antibodies

    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: 0-50 μM
    Incubation Time: 4 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: MCF-7 cells
    Concentration: 0-40 μM
    Incubation Time: 72 hours
    Result: Inhibited phosphorylation of CDK7 substrates.

    Apoptosis Analysis[1]

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

    BS-181 (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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

    380.53

    Appearance

    Solid

    Formula

    C22H32N6
    CAS No.
    SMILES

    CC(C1=C(N=C(C=C2NCC3=CC=CC=C3)NCCCCCCN)N2N=C1)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (131.40 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6279 mL 13.1396 mL 26.2791 mL
    5 mM 0.5256 mL 2.6279 mL 5.2558 mL
    10 mM 0.2628 mL 1.3140 mL 2.6279 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 3 mg/mL (7.88 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 3 mg/mL (7.88 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 3 mg/mL (7.88 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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    BS-181 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    BS-1811092443-52-1BS181BS 181CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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