Biochem/physiol Actions

Cell permeable: no

Reversible: yes

Target IC₅₀: 15 µM against phospholipase D

Product does not compete with ATP.

Primary Targetprotein tyrosine phosphatases

General description

An anti-neoplastic, anti-angiogenic agent that uncouples G-proteins from receptors presumably by blocking their interaction with intracellular receptor domains. A competitive inhibitor of reverse transcriptase. Reported to inhibit topoisomerase I and II. Inhibits Ca²⁺-ATPase in sarcoplasmic reticulum membranes. Also inhibits the cell-surface binding of various growth factors including EGF, PDGF, and TGF-β. An inhibitor of phospholipase D (IC₅₀ = 15 µM). Reported to interact with ATP-binding enzymes and P₂-purinergic receptors. An effective inhibitor of angiogenesis in calmodulin assays when given in combination with angiostatic steroids.

A reversible and competitive inhibitor of protein tyrosine phosphatases. An anti-neoplastic, anti-angiogenic agent that uncouples G-proteins from receptors presumably by blocking their interaction with intracellular receptor domains. Inhibits GDP-GTP exchange, the rate limiting step in the activation of G_α-subunits. A competitive inhibitor of reverse transcriptase. Reported to inhibit topoisomerases I and II. Inhibits Ca²⁺-ATPase in sarcoplasmic reticulum membranes. Also inhibits the cell-surface binding of various growth factors, including EGF, PDGF, and TGF-β. An inhibitor of phospholipase D (IC₅₀ = 15 µM). Reported to interact with ATP-binding enzymes and P₂-purinergic receptors. An effective inhibitor of angiogenesis in the calmodulin assay when given in combination with angiostatic steroids.

Legal Information

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

Other Notes

Meyers, M.O., et al. 2000. J. Surg. Res. 91, 130.Hohenegger, M., et al. 1998. Proc. Natl. Acad. Sci. USA 95, 346.Waldhoer, M., et al. 1998. Mol. Pharmacol. 53, 808.Zhang, Y.L., et al. 1998. J. Biol. Chem. 273, 12281.Hohenegger, M., et al. 1996. Mol. Pharmacol. 50, 1443.Emmick, J.J., et al. 1994. J. Pharmacol. Exp. Ther. 269, 717.Denhertog, A., et al. 1992. J. Physiol.454, 591.Nakajima, M., et al. 1991. J. Biol. Chem.266, 9661.Wilks, J.W., et al. 1991. Int. J. Radiat. Biol.60, 73.Huang, R.C., et al. 1990. Mol. Pharmacol.37, 304.Kopp, R. and Pfeiffer, A. 1990. Cancer Res.50, 6490.

Packaging

50 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)