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

Descrição detalhada : 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 p38alpha, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-alpha 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 37.5C., 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 p38alpha, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-alpha 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 37.5C.
Sinónimos : JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem; 5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
Fórmula molecula r: C5H3N5O2S3
Armazenamento : -20C
Embalagem : 1X10MG