Damnacanthal-CAS 477-84-9-Calbiochem

C₁₆H₁₀O₅

282.25

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.

Cell permeable: yes
Primary Target
p56^lck autophosphorylation
Target IC₅₀: 17 nM against p56lck autophosphorylation
Product does not compete with ATP.
Reversible: yes

Toxicity: Standard Handling (A)

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

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.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

orange-yellow

DMSO: 5 mg/mL

ambient

−20℃

1S/C16H10O5/c1-21-16-11(7-17)12(18)6-10-13(16)15(20)9-5-3-2-4-8(9)14(10)19/h2-7,18H,1H3

IPDMWUNUULAXLU-UHFFFAOYSA-N

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1