产品描述
| 熔点 | 255°C |
| 敏感性 | 对热敏感 |
| 溶解性 | Soluble in dimethyl sulfoxide at 100 mg/mL. |
| 存贮条件 | 储存温度:-20℃ |
| 密度 | 1.2300 |
| 产品介绍 | λmax 305(MeOH)(Lit.) A benzoquinoid antibiotic that inhibits p60c-src tyrosine kinase and c-myc gene expression in murine lymphoblastoma cells. Geldanamycin has antiproliferative and antitumor effects. Rapidly depletes p185c-erbB2 protein tyrosine kinase in breast carcinoma cells. Binds to HSP90 and disrupts Raf1-HSP90 complex leading to destabilization of Raf1. Inhibits basal and hypoxia-induced expression of c-Jun (IC50 = 75 nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase activity. Also known to selectively destabilize mutated p53 protein from a number of breast, leukemia, and prostate cell lines. A benzoquinoid antibiotic that is a potent inhibitor of pp60src tyrosine kinase. Geldanamycin has antiproliferative and antitumor effects. Inhibits basal and hypoxia-induced expression of c-Jun (IC50 = 75 nM) and abolishes hypoxia-induced increase in c-Jun N-terminal Kinase activity. Binds to HSP90 and disrupts raf1-HSP90 complex leading to destabilizing of Raf1. Also destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. Inhibits c-myc expression in murine lymphoblastoma cells. Approximately ten-fold more potent than herbimycin A |
| 生化机理 | 格尔德霉素是一种强效的抗肿瘤抗生素。在纳摩尔浓度级对60个细胞系具有活性。特异性结合热休克蛋白Hsp90和它的内质网同源物GP96，从而干扰了蛋白质的构象和细胞应激反应。此外，它是一种强效的核激素受体家族抑制剂。 |
| 别名 | 格尔德霉素;Streptomyces hygroscopicus - CAS 30562-34-6 - Calbiochem；NSC 122750 U-29135 |
