Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary Targetp56^lck autophosphorylation

Target IC₅₀: 17 nM against p56lck autophosphorylation

Cell permeable: yes

General description

A cell-permeable, potent, reversible, and selective inhibitor of p56^lck tyrosine kinase activity. Inhibits p56^lck autophosphorylation (IC₅₀ = 17 nM) and phosphorylation of an exogenous peptide by p56^lck over PKA and PKC and >40 fold selectivity for p56^lck over EGF, c-erbB2, insulin, and the PDGF receptor tyrosine kinases. In addition, damnacanthal exhibits 7-20 fold selectivity for p56^lck over pp60^src and pp59^fyn. Inhibition of p56^lck by damnacanthal appears to be reversible, not time-dependent and not significantly affected by the presence of sulfhydryl reagents. Also known to have antimalarial properties, and to reverse the phenotype of ras-transformed cells.

A cell-permeable, potent, reversible, and selective inhibitor of p56^lck tyrosine kinase. Inhibits p56^lck autophosphorylation (IC₅₀ = 17 nM) and phosphorylation of an exogenous peptide by p56^lck (IC₅₀ = 620 nM). Exhibits over 100-fold greater selectivity for p56^lck over PKA and PKC, 40-fold greater selectivity for p56^lck over EGF receptor kinase, c-ErbB2, insulin receptor kinase, and PDGF receptor kinase, and 7 - 20-fold greater selectivity for p56^lck over p60^src and p59^fyn. Inhibition of p56^lck is not significantly affected by the presence of sulfhydryl reagents. Also known to have antimalarial properties and to reverse the phenotype of ras-transformed cells.

Legal Information

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

Other Notes

Faltynek, C.R., et al. 1995. Biochemistry34, 12404.Hiramatsu, T., et al. 1993. Cancer Lett.73, 161.Koumaglo, K., et al. 1992. Planta Med.58, 533.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

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)