aladdin 阿拉丁 B286827 BI 78D3,JNK抑制剂 883065-90-5 ≥99%(HPLC)

中文名：BI 78D3,JNK抑制剂

英文名：BI 78D3

纯度：≥99%(HPLC)

货号：B286827

Cas号：883065-90-5

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

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.

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