zt-12-037-01

Description: ZT-12-037-01 is a novel, potent, ATP-competitive and specific STK19-targeted inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It can effectively block oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. It has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM. Activating mutations in NRAS account for 20%-30% of melanoma, but despite decades of research and in contrast to BRAF, no effective anti-NRAS therapies have been forthcoming.

References: Cell. 2019 Feb 21; 176(5):1113-1127.e16.