ZT-12-037-01

Product NameZT-12-037-01
CAS2328073-61-4
MFC21H31N5O2
MW385.5
EINECS
MOL File2328073-61-4.mol

Chemical Properties

storage temp.	2-8°C(protect from light)
solubility	DMSO: 8.33 mg/mL (21.61 mM)
form	Solid
color	White to off-white
InChI	1S/C21H31N5O2/c1-13(2)26-9-7-15(8-10-26)22-20-16-11-18(27-3)19(28-4)12-17(16)24-21(25-20)23-14-5-6-14/h11-15H,5-10H2,1-4H3,(H2,22,23,24,25)
InChIKey	AMAQJTHMSLYMFT-UHFFFAOYSA-N
SMILES	N1(CCC(CC1)Nc2nc(nc4c2cc(c(c4)OC)OC)NC3CC3)C(C)C

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

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

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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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Target	Value
STK19 (Cell-free assay)	23.96 nM
STK19 (D89N) (Cell-free assay)	27.94 nM