UNC0321 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂,Ki 为 63 pM,IC50 值为 6-9 nM。UNC0321 还抑制 GLP,IC50 值为 15-23 nM。UNC0321 对 SET7/9,SET8/PreSET7,PRMT3 和 JMJD2E 无活性。
In G9a ECSD and CLOT assays, the IC
50
values of 9 nM and 6 nM for UNC0321 (Compound 29), respectively. In GLP ECSD and CLOT assays, the IC
50
values of 15 nM and 23 nM for UNC0321, respectively.
UNC0321 (Compound 3) reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 11 μM.