Biological Activity
Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines. [5] Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6]. For the detailed information of Geldanamycin (NSC122750), the solubility of Geldanamycin (NSC122750) in water, the solubility of Geldanamycin (NSC122750) in DMSO, the solubility of Geldanamycin (NSC122750) in PBS buffer, the animal experiment (test) of Geldanamycin (NSC122750), the cell expriment (test) of Geldanamycin (NSC122750), the in vivo, in vitro and clinical trial test of Geldanamycin (NSC122750), the EC50, IC50,and affinity,of Geldanamycin (NSC122750), Please contact DC Chemicals.
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.











