ZT-12-037-01 (C007B-318504)

InformationZT-12-037-01 ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM.TargetsSTK19 (Cell-free assay); STK19 (D89N) (Cell-free assay) 23.96 nM; 27.94 nMIn vitroZT-12-037-01 treatment efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner. Furthermore, with increasing ATP concentrations, the IC50 of ZT-12-037-01 against STK19 accordingly increased, indicating that ZT-12-037-01 is an ATP-competitive inhibitor for STK19. ZT-12-037-01 treatment significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation, proliferation, and tumor formation. Pro-apoptotic effect of ZT-12-037-01 is dramatically enhanced in cells expressing oncogenic NRAS.In vivoZT-12-037-01 is a highly potent STK19 inhibitor with low in vivo toxicity. Its treatment also inhibits growth of SK-MEL-2 xenograft melanoma (with NRASQ61R) in a dose-dependent manner.Cell Research(from reference)Cell lines：A375, UACC62, SK-MEL-2 and WM2032 cells Concentrations：0 μM, 1 μM, or 3 μM Incubation Time：4 days. Specification: 0.99 Molecular Formula: C21H31N5O2 Molecular Weight: 385.5 PubChem CID: 138911316 Isomeric SMILES: CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OC)NC4CC4

UPC:

51112000

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

Z414230-25mg

CAS:

2328073-61-4

Product Size:

25mg