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375670

Sigma-Aldrich

Herbimycin A, Streptomyces sp.

A potent and cell-permeable protein tyrosine kinase inhibitor.

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

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

General description

A cell-permeable, potent inhibitor of protein tyrosine kinases. Inhibits p60v-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 p60v-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
P60v-src
Product does not compete with ATP.
Reversible: no
Target IC50: 12 µM against P60v-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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

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