Geldanamycin, Streptomyces hygroscopicus

A benzoquinoid antibiotic that inhibits p60^c-src tyrosine kinase and c-myc gene expression in murine lymphoblastoma cells. Geldanamycin has antiproliferative and antitumor effects. Rapidly depletes p185^c-erbB2 protein tyrosine kinase in breast carcinoma cells. Binds to HSP90 and disrupts Raf1-HSP90 complex leading to destabilization of Raf1. Inhibits basal and hypoxia-induced expression of c-Jun (IC₅₀ = 75 nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase activity. Also known to selectively destabilize mutated p53 protein from a number of breast, leukemia, and prostate cell lines.

A benzoquinoid antibiotic that is a potent inhibitor of pp60^src tyrosine kinase. Geldanamycin has antiproliferative and antitumor effects. Inhibits basal and hypoxia-induced expression of c-Jun (IC₅₀ = 75 nM) and abolishes hypoxia-induced increase in c-Jun N-terminal Kinase activity. Binds to HSP90 and disrupts raf1-HSP90 complex leading to destabilizing of Raf1. Also destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. Inhibits c-myc expression in murine lymphoblastoma cells. Approximately ten-fold more potent than herbimycin A (Cat. No. 375670).

Cell permeable: no

Primary Target
pc60^c-svc tyrosine kinase

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 75 nM Inhibiting basal and hypoxia-induced expression of c-Jun

Toxicity: Standard Handling (A)

Further dilute with aqueous buffers just prior to use.

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