An Hsp90 inhibitor (IC50 = 2 mM for Hsp90 ATPase activity); inhibits growth of 38 cancer cell lines (mean IC50 = 0.4 mM); induces dose-dependent degradation of the Hsp90 client proteins ErbB2 and cRaf1; inhibits tumor growth and delays disease progression in DU145 xenograft model

Macbecin I – 1 mg

Brand:
Cayman
CAS:
73341-72-7
Storage:
-20
UN-No:
Non-Hazardous - /

Macbecin I is a benzoquinone ansamycin antibiotic that binds to and inhibits heat shock protein 90 (Hsp90) in vitro (IC50 = 2 mM for Hsp90 ATPase activity).{34755} Macbecin I inhibits growth of 38 cancer cell lines (mean IC50 = 0.4 mM), with prostate DU145 cells being the most sensitive (IC70 < 0.01 mM). DU145 cells treated with macbecin I (1-10 mM) show dose-dependent degradation of the Hsp90 client proteins ErbB2 and cRaf1, consistent with the mechanism of Hsp90 inhibition. Macbecin I, at a dose of 10 mg/kg, inhibits tumor growth and delays disease progression in a human prostate carcinoma DU145 xenograft model.  

 

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Description

An Hsp90 inhibitor (IC50 = 2 mM for Hsp90 ATPase activity); inhibits growth of 38 cancer cell lines (mean IC50 = 0.4 mM); induces dose-dependent degradation of the Hsp90 client proteins ErbB2 and cRaf1; inhibits tumor growth and delays disease progression in DU145 xenograft model

Formal name: 6,17-didemethoxy-15R-methoxy-6-methyl-11-O-methyl-geldanamycin

Synonyms:  (+)-Macbecin|NSC 330499

Molecular weight: 558.7

CAS: 73341-72-7

Purity: ≥95%

Formulation: A lyophilized solid

Product Type|Biochemicals|Small Molecule Inhibitors|Heat Shock Proteins||Research Area|Cancer||Research Area|Cell Biology|Cellular Chaperones

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