ZT-12-037-01

Catalog No.S8864

For research use only.

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

CAS No. 2328073-61-4

Purity & Quality Control

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

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].

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].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: A375, UACC62, SK-MEL-2 and WM2032 cells
  • Concentrations: 0 μM, 1 μM, or 3 μM
  • Incubation Time: 4 days
  • Method:

    --

Animal Research:

[1]

  • Animal Models: C57BL/6J mice
  • Dosages: 25 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

DMSO 41 mg/mL
(106.35 mM)
Ethanol 3 mg/mL
(7.78 mM)
Water Insoluble

Chemical Information

Molecular Weight 385.50
Formula

C21H31N5O2

CAS No. 2328073-61-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OC)NC4CC4

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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