Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase with IC50 of 17 nM for inhibition of p56lck autophosphorylation.
Damnacanthal also shows an IC50 of 620 nM for phosphorylation of an exogenous peptide by p56lck.
Damnacanthal displays >100-fold selectivity over PKA and PKC, modest (7-20-fold) over p60src and p59fyn.
Damnacanthal inhibits PMACI-induced IL-1β, IL-6 and TNF-α expressions by suppressing NF-κB activation and suppresses the activation of caspase-1 and the expression of RIP-2 in mast cells.
Damnacanthal also is an effective inhibitor of LIMK1/2 (IC50=0.8/1.53 uM, respectively).
