375670

Herbimycin A, Streptomyces sp.

A potent and cell-permeable protein tyrosine kinase inhibitor.

• Sinônimo(s): Herbimycin A, Streptomyces sp.
• Fórmula empírica (Notação de Hill): C₃₀H₄₂N₂O₉
• Número CAS: 70563-58-5
• Peso molecular: 574.66
• Número MDL: MFCD00151702
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 1 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

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.

A potent and cell-permeable protein tyrosine kinase inhibitor. Inhibits p60^v-src(IC₅₀ = 12 µM) and PDGF-induced phospholipase D activation (IC₅₀ = 8 µg/ml). Reported to inhibit c-Src related bone resorption (IC₅₀ = 70 nM). Inhibits angiogenesis in chick chorioallantoic membrane. Also shown to inhibit anti-CD3 monoclonal antibody-induced apoptosis of thymocytes.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
P60^v-src

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 µM against P60^v-src

Advertência

Toxicity: Carcinogenic / Teratogenic (D)

Nota de preparo

Further dilute with H₂O or aqueous buffers just prior to use.

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.

Outras notas

Fan, T.-P., et al. 1995. Trends Pharmacol. Sci. 16, 57.
Kim, B.Y. 1995. Biochem. Biophys. Res. Commun.212, 1061.
Migita, K., et al. 1994. J. Immunol.153, 3457.
Okabe, M., et al. 1994. Leuk. Res. 18, 867.
Fukazawa, H., et al. 1991. Biochem. Pharmacol.42, 1661.
Obinata, A., et al. 1991. Exp. Cell Res.193, 36.
Park, D.J., et al. 1991. J. Biol. Chem.266, 24237.
Weinstein, S.L., et al. 1991. Proc. Natl. Acad. Sci. USA88, 4148.
Oikawa, T., et al. 1989. Cancer Lett.48, 157.
Uehara, Y., et al. 1989. Biochem. Biophys. Res. Commun.163, 803.
Uehara, Y., et al. 1988. Virology164, 294.
Omura, S., et al. 1979. J. Antibiotics32, 255.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3