375670

Herbimycin A, Streptomyces sp.

A potent and cell-permeable protein tyrosine kinase inhibitor.

• 동의어(들): Herbimycin A, Streptomyces sp.
• 실험식(Hill 표기법): C₃₀H₄₂N₂O₉
• CAS Number: 70563-58-5
• Molecular Weight: 574.66
• MDL number: MFCD00151702
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: yellow
• solubility: DMSO: 1 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
P60^v-src

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12 µM against P60^v-src

경고

Toxicity: Carcinogenic / Teratogenic (D)

제조 메모

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

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

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