Home Apoptosis Serine/threonin kinase inhibitor ZT-12-037-01

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ZT-12-037-01 Serine/threonin kinase inhibitor

Cat.No.S8864

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 Serine/threonin kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 385.50

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 385.50 Formula

C21H31N5O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2328073-61-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OC)NC4CC4

Solubility

In vitro
Batch:

DMSO : 41 mg/mL (106.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
STK19 [1]
(Cell-free assay)
23.96 nM
STK19 (D89N) [1]
(Cell-free assay)
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 this compound against STK19 accordingly increased, indicating that it is an ATP-competitive inhibitor for STK19. This chemical treatment significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation, proliferation, and tumor formation. Pro-apoptotic effect of the compound 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].
References

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