产品描述:
WM-3835 is an inhibitor of lysine acetyltransferase 6A (KAT6A) and KAT7 (IC50s = 17 and 30 nM, respectively).{51693} It is selective for KAT6A and KAT7 over KAT5 (IC50 = 312 nM). WM-3835 (1 µM) reduces the viability of primary mouse leukemia stem cells (LSCs), MOLM-13 and OCI-AML-3 acute myeloid lymphoma (AML) cells, as well as decreases colony formation in patient-derived primary AML cells. It induces cell cycle arrest at the sub-G1 phase and apoptosis, as well as decreases the levels of mRNA encoding homeobox protein A7 (HOXA7), in MOLM-13 cells. In vivo, WM-3835 (5 mg/kg per day) reduces tumor volume, weight, and growth rate, as well as decreases the acetylation at lysine 14 on histone 3 (H3K14), H3K12, and H3K5 in tumor cell lysates, in a PPC-1 prostate cancer mouse xenograft model.{51694}