化合物GSK872 T4074

Product Introduction
Bioactivity


英文名: GSK-872

描述: GSK-872 (GSK2399872A) 是一种有效且特异性的 RIP3 激酶抑制剂，降低 RIPK3 介导的坏死和随后的 HMGB1 的细胞质易位和表达，可改善早期脑损伤中的脑水肿和神经功能缺损。它以高亲和力结合 RIP3 激酶结构域，IC50为1.8 nM，并抑制激酶活性，IC50为1.3 nM。

体外活性: GSK872 (1 μM) has no inhibition for most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase. In HT-29 cells, GSK872 concentration-dependently blocks TNF-induced necroptosis. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK872 inhibits DAI- or TLR3-induced (RIP1-independent) death. It induces caspase activation and then induces apoptotic cell death[1].

体内活性: In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression [3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 71 mg/mL (185.1 mM)
Ethanol : 38 mg/mL (99.1 mM)


关键字: translocation | neurological | HMGB1 | Receptor-interacting protein kinases | brain | GSK 872 | GSK-872 | cytoplasmic | deficits | Inhibitor | edema | inhibit | RIPK | RIP kinase

相关产品: RIPK1-IN-9 | Necroptosis-IN-1 | SZM-1209 | RIPK1-IN-7 | PK68 | HS-1371 | Necrostatin-5 | Necrostatin-1 | GSK481 | GSK2983559 free acid

相关库: Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | NF-κB Signaling Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Antidepressant Compound Library | Inhibitor Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途