ACBI1

一种PROTAC，可驱动BRM、BRG1和PBRM1降解（在MV4-11细胞中DC50s分别为6、11和32nM）；降低MV4-11细胞的增殖（IC50=28nM），但对BRM和BRG1缺陷的NCI H1703细胞无效；可防止50和100nM时分离的人类CD8+T细胞耗竭。A PROTAC that drives BRM, BRG1, and PBRM1 degradation (DC50s = 6, 11, and 32 nM, respectively, in MV4-11 cells); decreases the proliferation of MV4-11 cells (IC50 = 28 nM) but is inactive against BRM- and BRG1-deficient NCI H1703 cells; prevents exhaustion of isolated human CD8+ T cells at 50 and 100 nM.分子式C49H58FN9O7S分子量936.1NC1=C(N2CCN(CC2)CC3=CC=C(C=C3)OCCOC4=C(C=CC(C5=C(N=CS5)C)=C4)CNC([C@H]6N(C[C@@H](C6)O)C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)=O)C=C(C8=C(C=CC=C8)O)N=N1