ZT-12-037-01 Chemical Properties,Usage,Production
Uses
ZT-12-037-01 is a STK19-targeted inhibitor, 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[1].
Biological Activity
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.
target
| Target | Value |
STK19 (Cell-free assay) | 23.96 nM |
STK19 (D89N) (Cell-free assay) | 27.94 nM |
< /table>
References
[1] Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16. DOI:10.1016/j.cell.2019.01.002
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2328073-61-4, ZT-12-037-01Related Search:
ZT-12-037-01
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