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

C₅H₃N₅O₂S₃

261.30

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.

Toxicity: Standard Handling (A)

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

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

pale yellow

ethanol: 4 mg/mL
DMSO: 50 mg/mL

wet ice

−20℃

Packaged under inert gas

11 - Combustible Solids

WGK 3