Cell-permeable, potent, selective, Ac-CoA competitive and reversible inhibitor of HBO1, KAT6A, and TIP60 acetyltransferases
WM-3835is a cell-permeable hydroxybenzenesulfonohydrazide compound that 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.).
Acute myeloid leukaemia (AML) is a heterogeneous disease characterized by transcriptional dysregulation that results in a block in differentiation and increased malignant self-renewal. Various epigenetic therapies aimed at reversing these hallmarks of AML have progressed into clinical trials, but most
HBO1 (KAT7 or MYST2) is a histone acetyltransferase that acetylates H3 and H4 histones. Methods: HBO1 expression was tested in human OS tissues and cells. Genetic strategies, including shRNA, CRISPR/Cas9 and overexpression constructs, were applied to exogenously alter HBO1 expression
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