Biochem/physiol Actions

Primary TargetHsp90

Cell permeable: no

Reversible: no

Product does not compete with ATP.

EC50 = 7.2 µM for Hsp90

General description

A less toxic, potent, synthetic derivative of the ansamycin benzoquinone antibiotic Geldanamycin Streptomyces hygroscopicus (Cat. No. 345805) that binds to Hsp90 (EC₅₀ = 7.2 µM) and regulates its function. Reported to induce apoptosis and exhibit anti-tumor properties (IC₅₀ = 4.1 nM in SKBR3 and 5.2 nM in MCF7 cells). Depletes cancer cells of erbB-1, erbB-2 (EC₅₀ = 45 nM), mutant p53, (EC₅₀ = 62 nM), Raf-1 (EC₅₀ = 80 nM), and Akt. Hence, inhibits the Ras/Raf/MEK and PI3-Kinase signaling pathways. Shown to sensitize cancer cells to Paclitaxel (Cat. No. 580555) and Doxorubicin (Cat. No. 324380), and down-regulates vascular endothelial factor expression.

Legal Information

GRANUCULT is a registered trademark of Merck KGaA, Darmstadt, Germany

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Basso, A.D., et al. 2002. Oncogene21, 1159.Clarke, P.A., et al. 2002. Oncogene19, 4125.Clarke, P.A., et al. 2000. Oncogene19, 4125.Schulte, T.W., and Neckers, L.M. 1998. Cancer Chemother. Pharmacol.42, 273.Schnur, R.C., et al. 1995. J. Med. Chem.38, 3806.

Packaging

Packaged under inert gas

500 µg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)