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Geldanamycin

Geldanamycin is an inhibitor of heat shock protein 90 (HSP90) that exhibits antiviral, neuroprotective, and anticancer activities. Geldanamycin decreases viral titers and inflammation in animal models of Chikungunya virus infection. Geldanamycin also accelerates nerve regeneration and enhances functional recovery in animal models of nerve crush injury. Additionally, geldanamycin sensitizes various cancer cell lines to the effects of other co-administered chemotherapeutics.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18926331

Cas No.

30562-34-6

Purity

≥97%

Formula

C29H40N2O9

Formula Wt.

560.64

IUPAC Name

[(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6-hydroxy-5,11,21-trimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate

Synonym

BRN 1633093

Melting Point

265-268°C

Solubility

Soluble in DMSO.

Appearance

Yellow Powder

Rathore AP, Haystead T, Das PK, et al. Chikungunya virus nsP3 & nsP4 interacts with HSP-90 to promote virus replication: HSP-90 inhibitors reduce CHIKV infection and inflammation in vivo. Antiviral Res. 2014 Mar;103:7-16. PMID: 24388965.

Sun HH, Saheb-Al-Zamani M, Yan Y, et al. Geldanamycin accelerated peripheral nerve regeneration in comparison to FK-506 in vivo. Neuroscience. 2012 Oct 25;223:114-23. PMID: 22835622.

McNamara AV, Barclay M, Watson AJ, et al. Hsp90 inhibitors sensitise human colon cancer cells to topoisomerase I poisons by depletion of key anti-apoptotic and cell cycle checkpoint proteins. Biochem Pharmacol. 2012 Feb 1;83(3):355-67. PMID: 22138446.

ARQ 197