Kongensin A

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Kongensin A  纯度: ≥98.0%

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。

Kongensin A

Kongensin A Chemical Structure

CAS No. : 885315-96-8

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Kongensin A 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

374.47

Formula

C22H30O5

CAS 号

885315-96-8

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)

参考文献
  • [1]. Li D, et al. Natural Product Kongensin A is a Non-Canonical HSP90 Inhibitor that Blocks RIP3-dependent Necroptosis. Cell Chem Biol. 2016 Feb 18;23(2):257-266.

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