WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice[1].
WM-3835is a cell-permeable hydroxybenzenesulfonohydrazide compound th at acts as a potent, selective, Ac-CoA competitive and reversible inhibitor of HBO1, KAT6A, and TIP60 acetyltransferases (IC50 = 0.030, 0.017 and 0.312 μM, respectively). WM-3835 is non-cytotoxic, dose-dependently, and rapidly decreases H3K14Ac levels (IC50 = 0.341 μM) and inhibits AML cells growth (IC50 = 0.297 μM in Molm13). Induces apoptosis, downregulates HOXA and IL-6 expression and up-regulates ALB secretion and delays hepatocyte and hMPC senescence. WM-1385 potently inhibits POS-1 xenograft growth in SCID mice (10 mg/kg, i.p.).
