420144

JNK Inhibitor XIII

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(s): JNK Inhibitor XIII, 5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
• Empirical Formula (Hill Notation): C₅H₃N₅O₂S₃
• CAS Number: 40045-50-9
• Molecular Weight: 261.30
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pale yellow
• solubility: ethanol: 4 mg/mL; DMSO: 50 mg/mL
• shipped in: wet ice
• storage temp.: −20°C
• InChI: 1S/C5H3N5O2S3/c6-3-8-9-5(14-3)15-4-7-1-2(13-4)10(11)12/h1H,(H2,6,8)
• InChI key: NQQBNZBOOHHVQP-UHFFFAOYSA-N

Description

General description

A cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1_153-163) 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-JIP1_153-163) 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 Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable