中文名称:

KONGENSIN A

中文同义词:

英文名称:

Kongensin A

英文同义词:

Kongensin A

CAS号:

885315-96-8

分子式:

C22H30O5

分子量:

374.4706

EINECS号:

相关类别:

植物提取物;二萜

Mol文件:

885315-96-8.mol

生物活性

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。

靶点

HSP90 RIP3 Apoptosis

体外研究

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. Apoptosis Analysis 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 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.

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.

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.