Go 6983

Go 6983 is a protein kinase C (PKC) inhibitor with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCζ respectively. Go 6983 inhibited intracellular Ca(2+) accumulation, suggesting a mechanism for its vasodilator properties. In vitro, Go 6983 significantly inhibited antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. Go 6983 (100 nM) significantly reduced PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts (P < 0.01), and significantly inhibited superoxide release from PMNs by 90 +/- 2% (P < 0.01). Go 6983 attenuated post-I/R cardiac contractile dysfunction, which may be related in part to decreased superoxide production in the presence of PMNs.