HERBIMYCIN A Chemical Properties
- Melting point:229-231 °C
- Boiling point:752℃
- Density 1.19±0.1 g/cm3(Predicted)
- Flash point:>110°(230°F)
- storage temp. −20°C
- solubility DMSO: 7.5 mg/mL DMSO stock solution can be diluted in phosphate buffered saline. The ratio of buffer:DMSO should be greater than 500:1.
- form powder
- color yellow
- Sensitive Light Sensitive & Hygroscopic
- BRN 4834067
HERBIMYCIN A Usage And Synthesis
- UsesHerbimycin 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.
- UsesHerbimycin A is a benzoquinone ansamycin antibiotic from Streptomyces. It has herbicidal activity and acts as a cell-permeable inhibitor of non-receptor tyrosine kinases and the heat shock protein Hsp90. Herbimycin A inhibits Bcr-Abl with an IC50 value of 5 μM, a concentration that also effectively blocks Src, Yes, Fps, Ros, and ErbB but not protein kinases (PK) PKA, PKC, Rac, Myc, or Raf. Presumably through its effects on tyrosine kinase signaling, herbimycin A also impairs endothelial cell proliferation in the context of angiogenesis, NF-κB activation, phosphorylation of phospholipase C-γ1, and eggshell formation in schistosome parasites. Ansamycins, including herbimycin A and geldanamycin , bind Hsp90 and destabilize client proteins, including Src, Bcr-Abl, and ErbB2, leading to their ubiquitination and proteasomal degradation.
- DefinitionChEBI: A 19-membered macrocyle incorporating a benzoquinone ring and a lactam functionality. It is an ansamycin antibiotic that induces apoptosis and displays antitumour effects.
- Biological ActivityAnsamycin 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.
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