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GS-626510

Chemical Structure : GS-626510

CAS No.: 1637770-13-8

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GS-626510 (GS-6510;GS 6510;GS 626510)

Catalog No.: PC-70222Not For Human Use, Lab Use Only.

GS-626510 (GS-6510, GS 6510, GS 626510) is a novel BET family bromodomains inhibitor with Kd of 0.5-2.8 nM for BRD2/3/4, and BRDT.

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

    Biological Activity

    GS-626510 (GS-6510, GS 6510, GS 626510) is a novel BET family bromodomains inhibitor with Kd of 0.5-2.8 nM for BRD2/3/4, and BRDT; shows weak affinity for CREBBP and EP300 (Ki=170 and 220 nM); potently inhibits growth of RKO cells with IC50 of 33 nM, decreases MYC levels; TRIM33 is required for the ability of GS-626510 to maximally down-regulate MYC.

    Physicochemical Properties

    M.Wt 394.478
    Formula C25H22N4O
    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

    4-(2-cyclopropyl-7-(6-methylquinolin-5-yl)-1H-benzo[d]imidazol-5-yl)-3,5-dimethylisoxazole

    References

    1. Shi X, et al. Proc Natl Acad Sci U S A. 2016 Aug 2;113(31):E4558-66.

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