Lavendustin A - CAS 125697-92-9 - Calbiochem

General description

A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase (IC₅₀ = 11 nM) and p60^c-src (IC₅₀ = 500 nM) with little effect on protein kinase A or protein kinase C (IC₅₀ >200 µM). Also inhibits NMDA-stimulated cGMP production (IC₅₀ = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor (VEGF) in rats.

A cell-permeable, reversible, substrate competitive, and potent inhibitor of EGF receptor tyrosine kinase (IC₅₀ = 11 nM) and pp60^c-src (IC₅₀ = 500 nM) with little effect on protein kinase A or protein kinase C (IC₅₀ >200 µM). Also inhibits NMDA-stimulated cGMP production (IC₅₀ = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor in rats.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
EGF receptor tyrosine kinase

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 11 nM and 500 nM against EGF receptor tyrosine kinase and p60c-src, respectively

Warning

Toxicity: Standard Handling (A)

Preparation Note

Further dilute with aqueous buffer just prior to use.

Reconstitution

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

Other Notes

Hu, D.E., and Fan, T.-P. 1995. Br. J. Pharmacol. 114, 262.
Rodriguez, J., et al. 1994. Neuropharmacology 33, 1267.
Hsu, C.-Y., et al. 1991. J. Biol. Chem.266, 21105.
O’Dell, T.J., et al. 1991. Nature 353, 558; Onoda, T., et al. 1989. J. Nat. Prod.52, 1252.
Bishop, J.M. 1983. Annu. Rev. Biochem. 52, 307.

Legal Information

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