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Disarib

Chemical Structure : Disarib

CAS No.: 1998149-15-7

Disarib (BCL2-BAK inhibitor Disarib)

货号: PC-62553Not For Human Use, Lab Use Only.

Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members(BCL-xL, BCL2A1 etc.).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members (BCL-xL, BCL2A1 etc.).
    Disarib is a novel BCL2 inhibitor with a unique mechanism of BCL2 inhibition.
    Disarib shows selective cytotoxicity in BCL2 high cancer cell lines, and CLL patient primary cells, as compared to BCL2 low cell lines.
    Disarib induces apoptosis by disruption of BCL2-BAK interaction with Ki of 12.76 nM, but not that of BCL2-BAX or other members of the proapoptotic family such as PUMA and BIM, in vitro.
    Disarib abrogates tumor growth while sparing platelets, by activating intrinsic pathway of apoptosis.

    物理化学性质&存储条件

    分子量 547.855
    分子式 C26H16BrClN4OS
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    3-((2-(4-chlorobenzyl)-6-(4-bromophenyl)imidazo[2,1-b][1,3,4] -thiadiazol-5-yl)methylidene)-1,3-dihydro-2H-indol-2-one

    参考文献

    1. Iyer D, et al. FEBS J. 2016 Sep;283(18):3408-37.

    2. Vartak SV, et al. Biochem Pharmacol. 2016 Dec 15;122:10-22.

    3. Vartak SV, et al. Biochem Pharmacol. 2017 May 1;131:16-28. doi:

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