Kongensin A

Modify Date: 2024-01-09 17:41:24

Kongensin A Structure
Kongensin A structure
Common Name Kongensin A
CAS Number 885315-96-8 Molecular Weight 374.471
Density 1.2±0.1 g/cm3 Boiling Point 525.7±50.0 °C at 760 mmHg
Molecular Formula C22H30O5 Melting Point N/A
MSDS N/A Flash Point 178.4±23.6 °C

 Use of 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].

 Names

Name Kongensin A
Synonym More Synonyms

 Kongensin A Biological Activity

Description 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].
Related Catalog
Target

HSP90[1] RIP3[1] Apoptosis[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]. 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.
References

[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.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 525.7±50.0 °C at 760 mmHg
Molecular Formula C22H30O5
Molecular Weight 374.471
Flash Point 178.4±23.6 °C
Exact Mass 374.209320
PSA 80.67000
LogP 2.77
Vapour Pressure 0.0±3.1 mmHg at 25°C
Index of Refraction 1.542

 Safety Information

Hazard Codes Xi

 Synonyms

10,7-Metheno-7H-benzocycloundecene-8,13-dione, 1-(acetyloxy)-1,2,3,4,4a,5,6,9,10,11,12,13a-dodecahydro-6-hydroxy-4,4,13a-trimethyl-9-methylene-, (1R,4aR,6R,10R,13aS)-
(2R,4R,8R,9S,13R)-2-Hydroxy-5,5,9-trimethyl-14-methylene-10,15-dioxotricyclo[11.2.1.0]hexadec-1(16)-en-8-yl acetate
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