375670

Herbimycin A, Streptomyces sp.

A potent and cell-permeable protein tyrosine kinase inhibitor.

• Synonym(s): Herbimycin A, Streptomyces sp.
• Empirical Formula (Hill Notation): C₃₀H₄₂N₂O₉
• CAS Number: 70563-58-5
• Molecular Weight: 574.66
• MDL number: MFCD00151702
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 1 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
P60^v-src

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 µM against P60^v-src

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Preparation Note

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

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3