X1 compound
目录号 : GC26082X1 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
Sample solution is provided at 25 µL, 10mM.
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]。
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: |
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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