A natural inhibitor of p23 chaperone function; inhibits Hsp90 expression in vitro in NTERA-2 cells at 5 µg/ml; binds to and blocks p23 to induce apoptosis in HeLa-PRB cells (20 µM); inhibits breast cancer cell proliferation in vitro (IC50s = 8.84 and 3.22 µM in MCF-7 and SKBr-3 cells

Gedunin – 1 mg

Brand:
Cayman
CAS:
2753-30-2
Storage:
-20
UN-No:
Non-Hazardous - /

Gedunin is a natural inhibitor of the heat shock protein (Hsp90; Item Nos. 22734 | 22735) co-chaperone p23 that also inhibits Hsp90 expression in human teratocarcinomal NTERA-2 cells in vitro at 5 µg/ml.{35153} This tetranortriterpenoid, which is isolated from A. indica, binds to and blocks the chaperone activity of p23 to induce apoptosis in HeLa-PRB cells in vitro at a concentration of 20 µM.{35151} Gedunin inhibits breast cancer cell proliferation in vitro, with IC50 values of 8.84 and 3.22 µM in MCF-7 and SKBr-3 cells, respectively, and inhibits the growth of PANC-1 pancreatic cancer cells (IC50 = 25 µM) by targeting the sonic hedgehog pathway to induce apoptosis.{35147,35152} It also exerts anti-inflammatory effects in vivo. In a mouse model of articular inflammation induced by zymosan (Item No. 21175), gedunin (0.05-0.5 mg/kg, i.p.) reduces edema formation and the production of inflammatory cytokines.{35149} Gedunin (0.5 mg/kg) also inhibits the pleural accumulation of eosinophils and activated T lymphocytes in an ovalbumin-sensitized mouse model of allergic inflammation when administered prior to ovalbumin rechallenge.{35150} It also targets the lipopolysaccharide binding site and thus blocks Toll-like receptor 4 (TLR4) signaling in macrophages in vitro at a concentration of 10 µM.{35145}  

 

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Description

A natural inhibitor of p23 chaperone function; inhibits Hsp90 expression in vitro in NTERA-2 cells at 5 µg/ml; binds to and blocks p23 to induce apoptosis in HeLa-PRB cells (20 µM); inhibits breast cancer cell proliferation in vitro (IC50s = 8.84 and 3.22 µM in MCF-7 and SKBr-3 cells, respectively); inhibits PANC-1 pancreatic cancer cell growth in vitro (IC50 = 25 µM); has anti-inflammatory effects in mouse models of articular inflammation when used at doses of 0.05–0.5 mg/kg and allergic inflammation when used at a dose of 0.5 mg/kg; targets LPS binding and TLR4 signaling in macrophages when used at a concentration of 10 µM

Formal name: (1S,3aS,4aR,4bS,5R,6aR,10aR,10bR,12aS)-5-(acetyloxy)-1-(3-furanyl)-1,5,6,6a,7,10a,10b,11,12,12a-decahydro-4b,7,7,10a,12a-pentamethyl-oxireno[c]phenanthro[1,2-d]pyran-3,8(3aH,4bH)-dione

Synonyms:  NSC 113497

Molecular weight: 482.6

CAS: 2753-30-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Hedgehog Signaling||Research Area|Cell Biology|Cellular Chaperones||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity|Pattern Recognition

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