UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂,IC50 值为 4 nM。UNC 0631 有效降低 MDA-MB-231 细胞中 H3K9me2 的水平,IC50 为 25 nM。
UNC 0631 (Compound 7) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC 0631 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC 0631 reduces H3K9me2 levels with ICW IC
50
values of 25 nM, 18 nM, 26 nM, 24 nM, 51 nM, 72 nM and 46 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53
-/-
and IMR90 cell lines, respectively.