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Chemical Structure : XS018661
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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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.
| M.Wt | 392.46 | |
| Formula | C22H24N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Christott T, et al. SLAS Discov. 2019 Feb;24(2):133-141.
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