HERBIMYCIN A

Использование

Herbimycin A is the major analogue of a complex of benzoquinone ansamycin antibiotics isolated from a Streptomyces hygroscopicus. Herbimycin A inhibits the 90-kDa heat-shock protein (Hsp90) which provides essential chaperone support to various signal transduction molecules, including certain steroid hormone receptors and select kinases. Herbimycin also inhibits protein tyrosine kinase and angiogenesis.

Определение

ChEBI: A 19-membered macrocyle incorporating a benzoquinone ring and a lactam functionality. It is an ansamycin antibiotic that induces apoptosis and displays antitumour effects.

Общее описание

A cell-permeable, potent inhibitor of protein tyrosine kinases. Inhibits p60^v-src (IC₅₀ = 12 μM) autophosphorylation. Irreversibly binds to the sulfhydryl groups of the kinase. Dose-dependently inhibits PDGF-induced phospholipase D activation (IC₅₀ = 8 μg/ml). Also, reported to inhibit c-src related bone resorption (IC₅₀ = 70 nM). Inhibits angiogenesis in chick chorioallantoic membrane and blocks anti-CD3 monoclonal antibody-induced apoptosis of thymocytes. Several mammalian cell lines transformed with tyrosine kinase oncogenes (src, abl, fps, ros, yes, erbB) show reversion from the transformed to the normal phenotype after treatment with herbimycin A.

Биологическая активность

Ansamycin antibiotic that acts as a Src family kinase inhibitor. Binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL . Exhibits antiangiogenic activity in endothelial cells in vitro . Also inhibits Hsp90 and impairs recovery from heat shock.