FITC-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 is specifically a novel geldanamycin fluorescent probe that may be used in a fluorescence polarization assay for Hsp90 inhibitors (4). May also be used for detection of cell surface Hsp90 (5). Other geldanamycin fluorophores (BODPY) have been reported andused in FP HTS assays (6,7).

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. Llauger-Bufi L., et al. (2003) Bioorg. Med. Chem. Lett. 13: 3975.

6. Kim J., et al. (2006) J. Biomol. Screen 9: 375.

7. Gooljarsingh L.T. et al.(2006) Proc. Natl. Acad. Sci. USA 103: 7625.