Drug intelligence / Profile preview

WM-1119

Development stage
Preclinical
Lead developer
Monash University
Modality
Small Molecules
Administration
Oral
01

Overview

WM-1119 is a potent, selective, and orally bioavailable small molecule inhibitor of the MYST family lysine acetyltransferases KAT6A (MOZ) and KAT6B (MORF). It functions as a reversible competitor of acetyl coenzyme A (Ac-CoA), binding to the Ac-CoA binding site to inhibit histone acetylation. Preclinical studies have shown that WM-1119 induces cellular senescence and cell cycle arrest at the G1/S restriction point, particularly in INK4A/ARF-dependent pathways, without causing DNA damage. It has demonstrated significant anti-tumor activity in models of acute myeloid leukemia (AML), lymphoma, and hepatocellular carcinoma. Additionally, WM-1119 has been explored for its ability to suppress IgE-mediated mast cell activation and allergic inflammation by reducing AP-1 signaling and histone acetylation at the Fos promoter.

02

Targets

KAT7 (Lysine acetyltransferase 7)KAT6A (Lysine acetyltransferase 6A)KAT6B (Histone acetyltransferase KAT6B)KAT5 (Lysine acetyltransferase 5)

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