货号：G1085

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. Geldanamycin is the first class of HSP90 inhibitor with a Kd value of 1.2 µM and IC50<2μM for ATPase activity of Hsp90. Treatment with geldanamycin at concentration of 0.5μM or 1μM for 24h reduced the protein level of AKT, as well as Raf-1 and its downstream p-MEK1/2, but not N-Ras or MEK1/2 in SH-SY5Y cells. Geldanamycin at concentration of 1μM for 48h could induce apoptosis in several neuroblastoma cell lines, including SH-SY5Y, SK-N-SH and LAN-1 cells. Intraperitoneal administration of geldanamycin (10 mg/kg) ameliorated ICH-induced increase of brain water content significantly, improved the neurological outcome and had a neuroprotective effect after ICH.

作用机制

Geldanamycin can bind to the N-terminal ATP/ADP-binding domain of Hsp90 and minhibit the inherent ATPase activity of Hsp90.

产品信息