SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a K d value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing.
性状
Solid
体外研究(In Vitro)
SPEN-IN-1 (0-100 μM) 抑制 RepA-PRC2 和 RepA-SPEN,IC50 值分别为 30 和 48 μM。SPEN-IN-1 抑制 RepA、PRC2 和 SPEN,Kd 值分别为 400、47 和 420 nM。SPEN-IN-1 在体外和细胞内选择性地破坏 Xist 与同源蛋白的相互作用。SPEN-IN-1 强烈抑制 H3K27me3 和 PRC2 的积累。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
SPEN-IN-1 减少 RepA-SPEN 的体内相互作用。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Aguilar R, et al. Targeting Xist with compounds that disrupt RNA structure and X inactivation. Nature. 2022 Apr;604(7904):160-166.
溶解度数据
In Vitro: DMSO : 66.67 mg/mL (160.08 mM; Need ultrasonic)配制储备液