Biochem/physiol Actions

Reversible: yes

Primary Targetp56^lck tyrosine kinase

Product does not compete with ATP.

Cell permeable: yes

Target IC₅₀: 18.5 µM against p56lck tyrosine kinase

General description

A cell-permeable, reversible, substrate competitive and potent p56^lck tyrosine kinase inhibitor (IC₅₀ = 18.5 µM). Selectively blocks the growth of v-ras transformed human bronchial epithelial cells (IC₅₀ = 14.8 µM) without affecting normal human bronchial epithelial cells, even at a concentration of 370 mM. Reported to act as an inhibitor of Tau aggregation and aid in the disassembly of PHF in vitro and in vivo.

A cell-permeable, reversible, substrate competitive and potent p56^lck tyrosine kinase inhibitor (IC₅₀ = 18.5 µM). Selectively blocks the growth of v-ras transformed human bronchial epithelial cells (IC₅₀ = 15 µM). Also suppresses HER2/neu tyrosine kinase activity in HER2/neu overexpressing breast cancer cells.

Legal Information

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

Other Notes

Pickhardt, M., et al. 2004. J. Biol. Chem.280, 3628.Zhang, L., and Hung. M.C. 1996. Oncogene 12, 571.Chan, T.C., et al. 1993. Biochem. Biophys. Res. Commun. 193, 1152.Jayasuriya, H., et al. 1992. J. Nat. Prod.55, 696.

Packaging

50 mg in Glass bottle

Reconstitution

Following reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 3 months at -20°C. Unstable in aqueous alkali; reconstitute just prior to use.

Warning

Toxicity: Standard Handling (A)