耗材描述
Kongensin A
产品活性:Kongensin A 是一种从 Croton kongensis 中分离的天然产物。 Kongensin A 是一种有效的,共价的 HSP90 抑制剂,可阻断 RIP3 依赖性坏死病。Kongensin A 是一种有效的坏死性抑制剂和凋亡诱导剂,并具有潜在的抗坏死性和消炎性应用。
产品来源: https://www.medchemexpress.cn/kongensin-a.html
研究领域:Cell Cycle/DNA Damage | Metabolic Enzyme/Protease | Apoptosis
作用靶点:HSP | RIP kinase | Apoptosis | Necroptosis
来源:植物 | 大戟科 | 越南巴豆
In Vitro: Kongensin A (0-15 μM; 6 hours; HT29 cells) treatment induces caspase activation and apoptosis in multiple cancer cell lines in a dosage-dependent manner.
Kongensin A (0-15 μM; 24 hours; HT29 cells) treatment induces the degradation of RIPK1 and oncogenic kinases such as ERBB2, AKT, EGFR, and B-raf, and induces the up-regulation of HSP90A and HSP90B.
Kongensin A covalently binds to cysteine 420 in the middle domain of HSP90 and dissociates HSP90 from its cochaperone CDC37. The HSP90-CDC37 complex is required for RIP3 activation, KA blocks LPS/Smac mimetics/Z-VAD and RIP3 polymerization-induced cell death, in which cell death is dependent on RIP3 but not its upstream kinase RIP1.
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