NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimetlation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis.
References:
[1]. Lianhua Piao, et al. Discovery of potent small molecule inhibitors of histone lysine metltransferase NSDs. Eur J Med Chem. 2024 Feb 20:268:116264.
















