XS018661 | ENL/AF9 YEATS inhibitor | Probechem Biochemicals

Chemical Structure : XS018661

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XS018661 (XS 018661)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	392.46
分子式	C22H24N4O3
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	methyl 4-((2-(piperidin-1-ylmethyl)-1H-benzo[d]imidazol-5-yl)carbamoyl)benzoate

参考文献

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

XS018661 (XS 018661)

生物&药学活性

物理化学性质&存储条件

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XS018661 (XS 018661)

生物&药学活性

物理化学性质&存储条件

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