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Disarib

Chemical Structure : Disarib

CAS No.: 1998149-15-7

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Disarib (BCL2-BAK inhibitor Disarib)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 547.855
    Formula C26H16BrClN4OS
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

    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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