Yellow solid. PROTECT FROM LIGHT. A benzoquinoid antibiotic that inhibits p60c-src tyrosine kinase and c-myc gene expression in murine lymphoblastoma cells. Geldanamycin has antiproliferative and antitumor effects. Rapidly depletes p185c-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. Purity: ≥95% by HPLC. RTECS LX8920000, CAS 30562-34-6. Ref.: Vasilevskaya, I.A., and O’Dwyer, P.J. 1999. Cancer Res. 59, 3935. Mimnaugh, E.G., et al. 1996. J. Biol. Chem. 271, 22796. Schulte, T.W., et al. 1996. Mol. Cell. Biol. 16, 5839. Blagosklonny, M.V., et al. 1995. Oncogene 11, 933. Schnur, R.C., et al. 1995. J. Med. Chem. 38, 3806. Whitesell, L., et all. 1994. Proc. Natl. Acad. USA 91, 8324. Yamaki, H., et al. 1989. J. Antibiot. 42, 604. Uehara, Y., et al. 1984. Mol. Cell. Biol. 6, 2198. |
