产品说明
一般描述
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.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
其他说明
De, S.K., et al. 2009. J. Med. Chem.52, 1943.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C5H3N5O2S3 |
分子量 | 261.30 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | pale yellow |
溶解性 | ethanol: 4 mg/mL DMSO: 50 mg/mL |
运输 | wet ice |
储存温度 | −20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |