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Chemical Structure : Xist inhibitor X1
Catalog No.: PC-49693Not For Human Use, Lab Use Only.
Xist inhibitor X1 is a selective small molecule inhibitor of the non-coding RNA prototype Xist function, binds specifically to the RepA motif of Xist (Kd=0.4 uM) in vitro and in vivo.
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Xist inhibitor X1 is a selective small molecule inhibitor of the non-coding RNA prototype Xist function, binds specifically to the RepA motif of Xist (Kd=0.4 uM) in vitro and in vivo.
X1 disrupts the interaction between RepA and PRC2, reduces the affinity of RepA for PRC2 from a Kd of 47 to 420 nM (IC50 of 30 μM) and SPEN, and for SPEN from 76 to 717 nM (IC50 of 48 μM).
X1 specifically displaces two of Xist's required interacting protein partners, Polycomb repressive complex 2 (PRC2) and SPEN.
X1 did not inhibit the histone methyltransferase activity of PRC2 directly.
By interfering with PRC2 and SPEN interactions, X1 blocks histone H3 lysine‐27 trimethylation (H3K27me3) and abrogates the initiation of X‐chromosome inactivation.
X1 inhibits cell differentiation and growth in a female-specific manner.
| M.Wt | 416.48 | |
| Formula | C27H20N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Rodrigo Aguilar, et al. Nature. 2022 Apr;604(7904):160-166.
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