Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :Geldanamycin30562-34-6HY-15230560.C29H40N2O9>98%ySolubility:gDMSO ≥110mg/mL Water<1.2mg/mL Ethanol <1.2mg/mLMechanisms: Pathways:Cell Cycle/DNA Damage; Target:HSP Pathways:Metabolism/Protease; Target:HSP Biological Activity:Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 GeldanamycinisanaturalexistingHSP90inhibitorwithKdof12μM.M IC50 Value: 1.2 μM(Kd) Target: HSP90 in vitro: Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against thepanel of 60 human tumor cell lines. Geldanamycin causes a dose-dependent G2 arrest andreversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition isaccompanied by p53 increase and finally demonstrated to be p53 dependent. Geldanamycin causespolyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase andshows a IC50 with 70 nM. in vivo: Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levelsin FRE/erbB-2 mice....References:[1]. RIP1 mediates the protection of geldanamycin on neuronal injury induced by oxygen-glucosedeprivation combined with zVAD in primary cortical neurons By Chen, Wei-Wei; Yu, Hailong; Fan,Hong-Bin; Zhang, Cui-Cui; Zhang, Min; Zhang, Caiyi; Cheng, Yanbo; Kong J. Neurochem. (2012)120, 70-77. [2]. Li T, Ni S, Jia C, Wang H, Sun G, Wu L, Gan M, Shan G, He W, Lin L, Zhou H, Wang Y. Identification of 4,5-Dihydro-4-hydroxygeldanamycins As Shunt Products of GeldanamycinBiosynthesis. J Nat Prod. 2012 Jul 31. [3]. Sun HH, Saheb-Al-Zamani M, Yan Y, Hunter DA, Mackinnon SE, Johnson PJ. Geldanamycin accelerated peripheral nerve regeneration in comparison to FK-506 in vivo. Neuroscience. 2012 Jul 24. [4]WtFBtVMiBLitP. [4]. Wuest F, Bouvet V, Mai B, Lapointe PFluorine- and rhenium-containing geldanamycin derivatives as leads for the development ofmolecular probes for imaging ...Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
