Erbstatin

Erbstatin is an inhibitor of EGF receptor-associated tyrosine kinase that has been found in Streptomyces.^1,2 It is selective for EGF receptor-associated tyrosine kinase over protein kinase A (PKA) and PKC, but does inhibit phosphatidylinositol kinase (IC₅₀s = 0.2, 100, >179, and 25 µg/ml, respectively).¹ Erbstatin (10 µg/ml) induces apoptosis and DNA fragmentation in L1210 murine skin lymphocytic leukemia cells.² It inhibits LPS-induced production of prostaglandin F_2α (PGF_2α; Item Nos. 16010 | 16020) and nitrite in J774.2 macrophages in a concentration-dependent manner.³ Erbstatin (4 mg/animal) reduces tumor growth in an MCF-7 breast cancer mouse xenograft model when used in combination with the iron chelator foroxymithine, which prevents its degradation.⁴

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1. Onoda, T., Iinuma, H., Sasaki, Y., et al. Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J. Nat. Prod. 52(6), 1252-1257 (1989).

2. Simizu, S., Imoto, M., and Umezawa, K. Induction of apoptosis by erbstatin in mouse leukemia L1210 cells. Biosci. Biotech. Biochem. 58(9), 1549-1552 (1994).

3. Akarasereenont, P., Mitchell, J.A., Appleton, I., et al. Involvement of tyrosine kinase in the induction of cyclo-oxygenase and nitric oxide synthase by endotoxin in cultured cells. Br. J. Pharmacol. 113(4), 1522-1528 (1994).

4. Toi, M., Mukaida, H., Wada, T., et al. Antineoplastic effect of erbstatin on human mammary and esophageal tumors in athymic nude mice. Eur. J. Cancer 26(6), 722-724 (1990).