17-Allylaminogeldanamycin
Geldanamycin derivative 17-AAG is an inhibitor of heat shock protein 90 (HSP90) that exhibits anti-inflammatory, anticancer chemotherapeutic, and antiviral activities. In endothelial cells, 17-AAG induces degradation of IκBα, attenuating NF-κB activation. 17-AAG induces Bax-dependent apoptosis in a variety of cancer models, both in vitro as well as in vivo. Additionally, 17-AAG inhibits replication of human cytomegalovirus.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18831788
| Cas No. |
75747-14-7 |
|---|---|
| Purity |
≥97% |
| Formula |
C31H43N3O8 |
| Formula Wt. |
585.69 |
| IUPAC Name |
[(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate |
| Synonym |
17-(Allylamino)-17-desmethoxy-geldanamycin; allylaminogeldanamycin; 17-AAG; telatinib. |
| Melting Point |
200-205°C |
| Solubility |
Soluble in DMSO or methanol. |
| Appearance |
Purple powder |
product targets : ULK inhibitors
Thangjam GS, Dimitropoulou C, Joshi AD, et al. Novel mechanism of attenuation of LPS-induced NF-κB activation by the heat shock protein 90 inhibitor, 17-N-allylamino-17-demethoxygeldanamycin, in human lung microvascular endothelial cells. Am J Respir Cell Mol Biol. 2014 May;50(5):942-52. PMID: 24303801.
Powers MV, Valenti M, Miranda S, et al. Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX. Oncotarget. 2013 Nov;4(11):1963-75. PMID: 24185264.
Evers DL, Chao CF, Zhang Z, et al. 17-allylamino-17-(demethoxy)geldanamycin (17-AAG) is a potent and effective inhibitor of human cytomegalovirus replication in primary fibroblast cells. Arch Virol. 2012 Oct;157(10):1971-4. PMID: 22711259.
Gloesenkamp C, Nitzsche B, Lim AR, et al. Heat shock protein 90 is a promising target for effective growth inhibition of gastrointestinal neuroendocrine tumors. Int J Oncol. 2012 May;40(5):1659-67. PMID: 22246317.
