2 Biological Activity
17-AAG (Geldanamycin) is a less toxic analogue of the geldanamycin which binds to Hsp90 and alters its function. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, and oncogenesis. [1]
This agent displays a 100-fold higher affinity for HSP90 derived from tumor cells compared to HSP90 from normal cells. 17-AAG (Geldanamycin) binds into the ATP binding pocket in Hsp90 and induces the degradation of proteins that require this chaperone for conformational maturation. 17-AAG (Geldanamycin) inhibits Akt activation and expression in tumors and synergizes with a number of antitumor agents such as taxol, cisplatin, and UCN-014. [2]
3 References:
Synergism between Etoposide and 17-AAG in Leukemia Cells: Critical Roles for Hsp90, FLT3, Topoisomerase II, Chk1, and Rad51 Qing Yao, Brenda Weigel,et al. Clin Cancer Res 2007;13:1591-1600
Synergistic antileukemic interactions between 17-AAG and UCN-01 involve interruption of RAF/MEK- and AKT-related pathways Wentao Jia, Chunrong Yu,et al. Blood 2003;102: 1824-1832
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.