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biBET

Chemical Structure : biBET

CAS No.: 2059110-46-0

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biBET (BET bivalent inhibitor)

Catalog No.: PC-62224Not For Human Use, Lab Use Only.

biBET is a potent, selective, bivalent inhibitor of BET bromodomains with pKd of 8.3/7.3/11 for BRD4(1)/BRD4(2)/BRD4(1,2), respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    biBET is a potent, selective, bivalent inhibitor of BET bromodomains with pKd of 8.3/7.3/11 for BRD4(1)/BRD4(2)/BRD4(1,2), respectively.
    biBET exhibts very high cellular potency for BRD4 binding and pharmacological responses such as disruption of BRD4-mediator complex subunit 1 foci with an EC50 of 100 pM.
    biBET is an useful BET/BRD4 chemical probe.

    Physicochemical Properties

    M.Wt 530.593
    Formula C26H30N10O3
    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-Methoxy-N-(2-(4-(1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)-N-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-amine

    References

    1. Waring MJ, et al. Nat Chem Biol. 2016 Dec;12(12):1097-1104.

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