Kongensin A 

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].

HSP90^[1]
RIP3^[1]
Apoptosis^[1]

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.

374.47

C₂₂H₃₀O₅

885315-96-8

Solid

White to light yellow

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

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [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.  [Content Brief]