(15R)-17-デメトキシ-15-メトキシ-11-O-メチルゲルダナマイシン 化学特性,用途語,生産方法
外観
黄色の薄膜
溶解性
メタノール,DMSOに可溶。
用途
チロシンりん酸化の研究ツール。
使用
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.
定義
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.
一般的な説明
A cell-permeable, potent inhibitor of protein tyrosine kinases. Inhibits p60
v-src (IC
50 = 12 μM) autophosphorylation. Irreversibly binds to the sulfhydryl groups of the kinase. Dose-dependently inhibits PDGF-induced phospholipase D activation (IC
50 = 8 μg/ml). Also, reported to inhibit c-
src related bone resorption (IC
50 = 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.
生物活性
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.
(15R)-17-デメトキシ-15-メトキシ-11-O-メチルゲルダナマイシン 上流と下流の製品情報
原材料
準備製品