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XS018661

Chemical Structure : XS018661

CAS No.: 878415-59-9

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XS018661 (XS 018661)

Catalog No.: PC-20181Not For Human Use, Lab Use Only.

XS018661 (XS 018661) is a potent first-in-class inhibitor of the YEATS domains of ENL and AF9 with Kd of 754/523 nM, IC50 of 1.6/3.0 uM, respectively.

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

    Biological Activity

    XS018661 (XS 018661) is a potent first-in-class inhibitor of the YEATS domains of ENL and AF9 with Kd of 754/523 nM, IC50 of 1.6/3.0 uM, respectively.
    XS018661 showed no significant inhibition below 20 µM for a number of bromodomains (BRD4[first domain], BRD9, CECR2, CREBBP, FALZ, TAF1, and BAZ2B) at 20 uM.
    XS018661 demonstrate moderate cellular target engagement of XS018661 against AF9 in the micromolar range.
    A mutant of AF9 with a deficiency in the binding pocket (Y78A) was not significantly affected by XS018661.

    Physicochemical Properties

    M.Wt 392.46
    Formula C22H24N4O3
    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

    methyl 4-((2-(piperidin-1-ylmethyl)-1H-benzo[d]imidazol-5-yl)carbamoyl)benzoate

    References

    1. Christott T, et al. SLAS Discov. 2019 Feb;24(2):133-141.

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