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420144 Sigma-Aldrich

JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem

The JNK Inhibitor XIII, also referenced under CAS 40045-50-9, controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym: 5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine, JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem

  • CAS Number 40045-50-9

  • Empirical Formula (Hill Notation) C5H3N5O2S3

  • Molecular Weight 261.30

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology, Serine/Threonine Kinase Biology, Serine/Threonine Kinase Inhibitors,
Quality Level   100
assay   ≥95% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   pale yellow
solubility   ethanol: 4 mg/mL
  DMSO: 50 mg/mL
shipped in   wet ice

Description

General description

A cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1153-163) and TAT-pepJIP1 (Cat. Nos. 420133 & 420134, respectively) as a JIP-docking site-targeting (IC50 = 239 nM against pepJIP1 binding to JNK1) and substrate-competitive JNK inhibitor (IC50 = 700 nM against ATF2 phosphorylation by JNK1), while exhibiting little activity (IC50 >50 µM) toward p38α, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-α stimulation (IC50 = 6.23 µM) in vitro and restore insulin sensitivity in a murine of type-2 diabetes model (25 mg/kg, i.p.) in vivo. Biostability analysis with rat liver microsome preparations results in a compound half-life of 27 min at 37.5°C.

A cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1153-163) and TAT-pepJIP1 (Cat. Nos. 420133 & 420134, respectively) as a JIP-docking site-targeting (IC50 = 239 nM against pepJIP1 binding to JNK1) and substrate-competitive JNK inhibitor (IC50 = 700 nM against ATF2 phosphorylation by JNK1), while exhibiting little activity (IC50 >50 µM) toward p38α, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-α stimulation (IC50 = 6.23 µM) in vitro and restore insulin sensitivity in a murine of type-2 diabetes model (25 mg/kg, i.p.) in vivo. Biostability analysis with rat liver microsome preparations results in a compound half-life of 27 min at 37.5°C.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

De, S.K., et al. 2009. J. Med. Chem.52, 1943.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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