General description
A cell-permeable, potent, reversible, and selective inhibitor of p56lck tyrosine kinase. Inhibits p56lck autophosphorylation (IC50 = 17 nM) and phosphorylation of an exogenous peptide by p56lck (IC50 = 620 nM). Exhibits over 100-fold greater selectivity for p56lck over PKA and PKC, 40-fold greater selectivity for p56lck over EGF receptor kinase, c-ErbB2, insulin receptor kinase, and PDGF receptor kinase, and 7 - 20-fold greater selectivity for p56lck over p60src and p59fyn. Inhibition of p56lck 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.
A cell-permeable, potent, reversible, and selective inhibitor of p56lck tyrosine kinase activity. Inhibits p56lck autophosphorylation (IC50 = 17 nM) and phosphorylation of an exogenous peptide by p56lck over PKA and PKC and >40 fold selectivity for p56lck over EGF, c-erbB2, insulin, and the PDGF receptor tyrosine kinases. In addition, damnacanthal exhibits 7-20 fold selectivity for p56lck over pp60src and pp59fyn. Inhibition of p56lck 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p56lck autophosphorylation
Product does not compete with ATP.
Reversible: yes
Target IC50: 17 nM against p56lck autophosphorylation
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51283930
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 251650-1MG
