Home Apoptosis Serine/threonin kinase inhibitor ZT-12-037-01 For research use only.

ZT-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.

ZT-12-037-01 Chemical Structure

ZT-12-037-01 Chemical Structure

CAS: 2328073-61-4

Purity & Quality Control

Batch: S886401 DMSO] 41 mg/mL] false] Ethanol] 3 mg/mL] false] Water] Insoluble] false Purity: 99.58%
99.58

ZT-12-037-01 Related Products

Choose Selective Serine/threonin kinase Inhibitors

Biological Activity

Description 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.
Targets
STK19 [1]
(Cell-free assay)		 STK19 (D89N) [1]
(Cell-free assay)
23.96 nM 27.94 nM
In vitro
In vitro

ZT-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[1].
Cell Research Cell lines A375, UACC62, SK-MEL-2 and WM2032 cells
Concentrations 0 μM, 1 μM, or 3 μM
Incubation Time 4 days
Method

--
In Vivo
In vivo

ZT-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[1].
Animal Research Animal Models C57BL/6J mice
Dosages 25 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 385.50 Formula

C21H31N5O2
CAS No. 2328073-61-4 SDF --
Smiles CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OC)NC4CC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 41 mg/mL ( (106.35 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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