WM-1119 is a potent and selective inhibitor of the MYST family histone acetyltransferase (HAT) KAT6A (MOZ) – IC50 = 6.3 nM.1,2 Induces cell cycle exit and cellular senescence without causing DNA damage. WM-1119 repressed the cell proliferation of sorafenib-resistant hepatocellular carcinoma cells.3
References/Citations:
- Baell et al. (2018), Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth; Nature, 560 253
- Priebbenow et al. (2020), Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents; J. Med. Chem., 63 4655
- Jin et al. (2021), KAT6A is associated with sorafenib resistance and contributes to progression of hepatocellular carcinoma by targeting YAP; Biochem. Biophys. Res. Commun., 585 185
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