ZT-12-037-01 is an ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. At a concentration of 1 μM, it is highly selective against a kinase library of 468 kinases.
[in vitro]
Treatment with ZT-12-037-01 could effectively inhibit NRAS phosphorylation. ZT-12-037-01 is an ATP-competitive inhibitor that potently inhibits melanocytic colony formation, proliferation and tumor formation driven by mutant NRAS-STK19. It's pro-apoptotic activity was significantly enhanced in cells expressing oncogenic NRAS.
[in vivo]
ZT-12-037-01 is a potent STK19 inhibitor with low toxicity in vivo. In the SK-MEL-2 xenograft model (carrying NRAS.