[CAS NO. 885315-96-8] KongensinA
PRODUCTS SPECIFICATIONS [885315-96-8]
DESCRIPTION [885315-96-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 374.47 |
| Molecular Formula | C22H30O5 |
| 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 |
Summary
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] .
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]
.
MCE 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)