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X1 compound

目录号 : GC26082

X1 compound是非编码RNA原型Xist的RepA基序的高亲和力结合物,Kd值为0.4±0.3μM

X1 compound Chemical Structure

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5mg
¥2,121.00
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25mg
¥6,358.00
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Sample solution is provided at 25 µL, 10mM.

Description

X1 compound is a high-affinity binder to RepA motif of non-coding RNA prototype Xist with a Kd of 0.4±0.3μM. X1 compound shows progressively disruptive effects on RepA-PRC2 and RepA-SPEN interactions, with IC50 values of 30μM and 48μM, respectively and blocks initiation of X-chromosome inactivation. X1 compound exhibits inhibitory effects on cell growth and differentiation at a concentration of 5μM[1].

In vitro, 10 μM X1 compound treated female embryoid bodies (EB) derived from mouse ES cells with two active X chromosomes for 1-5 days inhibited cell differentiation and growth, with RepA-PRC2 and RepA-SPEN interaction inhibition observed on day2, and poor EB outgrowth, blunted H3K27me3 enrichment, and X-chromosome inactivation seen after 72 hours[1].

References:
[1] Aguilar R, Spencer KB, Kesner B,et al. Targeting Xist with compounds that disrupt RNA structure and X inactivation. Nature. 2022 Apr;604(7904):160-166

X1 compound是非编码RNA原型Xist的RepA基序的高亲和力结合物,Kd值为0.4±0.3μM。X1 compound对RepA-PRC2和RepA-SPEN的相互作用表现出抑制作用,IC50值分别为30μM和48μM,并阻断X染色体失活。X1 compound达到5μM时就可以表现出对细胞生长和分化的抑制作用[1]

在体外,10μM X1 compound处理携带活性X染色体的小鼠ES细胞的雌性胚状体(EB)1-5天,细胞分化和生长受到抑制,第2天观察到RepA-PRC2和RepA-SPEN相互作用被抑制,72小时后观察到EB生长不良,H3K27me3富集减弱,X染色体失活[1]

实验参考方法

Cell experiment [1]:

Cell lines

Mouse embryonic stem cells

Preparation Method

The female mouse embryonic stem (ES) cell model (TsixTST/+) initially carry two active X chromosome’s (Xa) but recapitulate X-chromosome inactivation when induced to differentiate into embryoid bodies (EB) for 4 days. The differentiation process was conducted with 10μM X1 compound on day 2 then the exposure was prolonged to day 7.

Reaction Conditions

10µM; 1-5 days

Applications

X1 compound treatment resulted in a female-specific inhibition of cell differentiation and growth by reducing RepA–PRC2 and RepA-SPEN interaction and blocking initiation of X-chromosome inactivation.

References:
[1] Aguilar R, Spencer KB, Kesner B,et al. Targeting Xist with compounds that disrupt RNA structure and X inactivation. Nature. 2022 Apr;604(7904):160-166

化学性质

Cas No. SDF Download SDF
分子式 C27H20N4O 分子量 416.48
溶解度 DMSO: 83 mg/mL (199.29 mM);Water: Insoluble;Ethanol: 20 mg/mL (48.02 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.4011 mL 12.0054 mL 24.0108 mL
5 mM 0.4802 mL 2.4011 mL 4.8022 mL
10 mM 0.2401 mL 1.2005 mL 2.4011 mL
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