BI 78D3
规格
| Cas Number | 883065-90-5 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 别名 | 4-(2,3-二氢-1,4-苯并二恶英-6-基)-2,4-二氢-5-[(5-硝基-2-噻唑基)硫基] -3H-1,2,4-三唑-3-一个 |
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 简短描述 | 选择性竞争性JNK抑制剂 |
| 英文简短描述 | Selective, competitive JNK inhibitor |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | 竞争性c-Jun N末端激酶（JNK）抑制剂（IC50 = 280 nM），其选择性比p38α高100倍以上，对mTOR和PI-3K无活性。抑制JNK相互作用蛋白1（JIP1）-JNK结合（IC50 = 500 nM），并防止JNK底物磷酸化。在II型糖尿病小鼠模型中，阻断JNK依赖性Con A诱导的肝损伤并恢复胰岛素敏感性。 |
| 英文描述 |
description： A cell-permeable benzodioxin-triazole compound that competes with JNK-interacting protein-1 (IC50 = 500 nM in competitive binding to JNK1 with pepJIP1) and D-domain-containing substrates binding (Ki = 200 nM in competitive binding to JNK1 with ATF2) by targeting JNK JIP1-interacting site (Kd = 8.1 µM). BI-78D3 inhibits the phosphorylation of ATF2, but not that of a D-domain-less peptide substrate, by JNK1 in kinase assays, while showing 100-fold less potency against p38α and no effect against mTOR or PI3-Kα. Shown to inhibit the TNF-α-stimulated GFP-cJun phosphorylation in transfected HeLa cultures in vitro (IC50 = 12.4 µM) and effectively reduce ConA-induced murine liver failure (10 mg/kg, i.p.) as well as restore insulin sensitivity in a murine type 2 diabetes model (25 mg/kg, i.p.) in vivo. |