Potent and selective, acetyl-CoA-competitive MYST family histone acetyltransferases KAT6A and KAT6B inhibitor with anti-cancer efficacy in vitro and in vivo.
WM-1119 is a potent and selective, acetyl coenzyme A (Acetyl-CoA)-competitive inhibitor against MYST family histone acetyltransferases KAT6A and KAT6B (KAT6B Kd = 2.1 nM by SPR, IC50 = 37 nM by activity assay; KAT7/5 Kd = 0.53/2.2 μM; no affinity toward 159 diverse biological targets). WM-1119 induces MEF G1 cell cycle arrest (1-10 μM), inhibits EMRK1184 lymphoma growth in cultures (IC50 = 250 nM) and in mice in vivo (50 mg/kg 3x or 4x i.p. per day).
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11 - Combustible Solids
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WGK 3
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Journal of medicinal chemistry, 63(9), 4655-4684 (2020-03-03)
A high-throughput screen designed to discover new inhibitors of histone acetyltransferase KAT6A uncovered CTX-0124143 (1), a unique aryl acylsulfonohydrazide with an IC50 of 1.0 μM. Using this acylsulfonohydrazide as a template, we herein disclose the results of our extensive structure-activity
Acetylation of histones by lysine acetyltransferases (KATs) is essential for chromatin organization and function1. Among the genes coding for the MYST family of KATs (KAT5-KAT8) are the oncogenes KAT6A (also known as MOZ) and KAT6B (also known as MORF and
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
CRISPR-based genetic screening has revolutionized cancer drug target discovery, yet reliable, multiplex gene editing to reveal synergies between gene targets remains a major challenge. Here, we present a simple and robust CRISPR-Cas12a-based approach for combinatorial genetic screening in cancer cells.
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