| Description | SPEN-IN-1 (compound X1) is a selective inhibitor of the SPEN protein factor, exhibiting a dissociation constant (K d) of 47 nM. Notably, it exhibits high specificity for RepA, a 431-nucleotide domain within Xist (a non-coding RNA prototype), characterized by 8.5 repeats of a GC-rich motif instrumental in gene silencing [1]. |
| In vitro | SPEN-IN-1 (0-100 μM) 对 RepA-PRC2 与 RepA-SPEN 均显示出抑制活性，其 IC50 分别为 30 μM 与 48 μM [1]。该化合物对 RepA、PRC2 及 SPEN 的 Kd 值分别为 400 nM、47 nM 及 420 nM [1]，并且它在体外和细胞层面特异性地阻断 Xist RNA 与其同源蛋白的结合 [1]。此外，SPEN-IN-1 显著抑制了 H3K27me3 的生成和 PRC2 的沉积 [1]。 |
| In vivo | SPEN-IN-1 降低了RepA-SPEN在体内的相互作用[1]。 |
| molecular weight | 416.47 |
| Molecular formula | C27H20N4O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |