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。
| 生物活性 | Kongensin A is a natural product isolated fromCroton kongensis. Kongensin A is an effective, covalentHSP90inhibitor that blocksRIP3-dependent necroptosishas. Kongensin A is a potentnecroptosisinhibitor and anapoptosisinducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications[1]. |
| IC50& Target | HSP90[1]
RIP3[1]
Apoptosis[1] |
体外研究
(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[1].
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[1].
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[1].
Apoptosis Analysis[1] | Cell Line: | HT29 cells | | Concentration: | 0 μM, 2.5 μM, 5 μM, 15 μM | | Incubation Time: | 6 hours | | Result: | Induced caspase activation and apoptosis in a dosage-dependent manner. |
Western Blot Analysis[1] | Cell Line: | HT29 cells | | Concentration: | 0 μM, 2.5 μM, 5 μM, 15 μM | | Incubation Time: | 24 hours | | Result: | Induced the degradation of RIPK1 and oncogenic kinases such as ERBB2, AKT, EGFR, and B-raf, and induced the up-regulation of HSP90A and HSP90B. |
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| 来源 | - Plants
- Euphorbiaceae
- Croton kongensisGagnep.
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
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