Biotin-Geldanamycin (Hsp90 Inhibitor)

Geldanamycin is a benzoquinoid ansamycin produced by Streptomyces hygroscopicus. It binds specifically to heat shock protein HSP90 and downregulates target proteins including tyrosine kinases, steroid receptors, transcription factors and cell cycle regulatory kinases (1,2). It induces the inactivation, destabilization and eventual degradation of HIF-1á (3).This inhibitor is a useful tool for affinity purification of HSP-90 and HSP-90 dependent client proteins (4).

1. Whitesell L., et al. (1994) Proc. Natl Acad. Sci. USA 91:8324.

2. Neckers L. (2002) Trends Mol. Med. 8: S55.

3. Mabjeesh N.J., et al. (2002) Cancer Res. 62: 2478.

4. Clevenger R.C. et al. (2004) J. Org. Chem. 69: 4375.