Description
General description
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 Gα-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.
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.
Biochem/physiol Actions
Cell permeable: no
Primary Target
protein tyrosine phosphatases
Product does not compete with ATP.
Reversible: yes
Target IC₅₀: 15 µM against phospholipase D
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
