半岛bd体育手机客户端 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 ?M) 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 ?M)in vitroand 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 ?M) 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 ?M)in vitroand 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 |
半岛bd体育手机客户端 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 |
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