375670

Herbimycin A, Streptomyces sp.

A potent and cell-permeable protein tyrosine kinase inhibitor.

• 别名: Herbimycin A, Streptomyces sp.
• 经验公式（希尔记法）: C₃₀H₄₂N₂O₉
• CAS号: 70563-58-5
• 分子量: 574.66
• MDL编号: MFCD00151702
• UNSPSC代码: 12352200

属性

• 质量水平: 100
• 方案: ≥95% (HPLC)
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: yellow
• 溶解性: DMSO: 1 mg/mL
• 运输: ambient
• 储存温度: −20°C

说明

一般描述

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.

生化/生理作用

Cell permeable: yes

Primary Target
P60^v-src

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 µM against P60^v-src

警告

Toxicity: Carcinogenic / Teratogenic (D)

制备说明

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

重悬

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

其他说明

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.

法律信息

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3