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.
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- Pureza: 98.0%
- No. CAS: 885315-96-8
- Fòrmula: C22H30O5
- Peso molecular:374.47
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Kongensin A
More
Actividad biológica
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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.
Chemical Information
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No. CAS 885315-96-8
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Appearance Solid
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Peso molecular 374.47
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)