Kongensin A
Based on 1 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 885315-96-8
- 分子式: C22H30O5
- 分子量:374.47
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
MedChemExpress(MCE)の使用を引用している文献 Kongensin A
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.12 μM
Compound: 8
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
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[PMID: 34236840] |
| MDA-MB-231 | IC50 |
0.177 μM
Compound: 8
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
|
[PMID: 34236840] |
| MDA-MB-468 | IC50 |
0.228 μM
Compound: 8
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Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 96 hrs by MTT method
|
[PMID: 34236840] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29 cells
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Concentration:0 μM, 2.5 μM, 5 μM, 15 μM
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Incubation Time:6 hours
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Result:Induced caspase activation and apoptosis in a dosage-dependent manner.
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Cell Line:HT29 cells
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Concentration:0 μM, 2.5 μM, 5 μM, 15 μM
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Incubation Time:24 hours
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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.
化学情報
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CAS 番号 885315-96-8
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性状 Solid
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分子量 374.47
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分子式 C22H30O5
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Color White to light yellow
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SMILES
C[C@]([C@@H](CC1)OC(C)=O)(C(CC[C@](C2=C)([H])C=C3C2=O)=O)[C@](C1(C)C)([H])C[C@H]3O
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Heliyon
Gkongensin A, an HSP90β inhibitor, improves hyperlipidemia, hepatic steatosis, and insulin resistance. [Abstract]2024 Apr 9;10(8):e29367. PMID: 38655315
純度とドキュメンテーション
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データシート (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)