Protein kinase inhibitor H-7 increases lipoprotein lipase activity in isolated rat fat pads.

A protein kinase inhibitor, 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H-7) increased lipoprotein lipase (LPL) activity in isolated rat fat pads in a time- and dose-dependent manner. The incubation of H-7 with partially purified LPL did not affect its activity. Under the marked inhibition of protein synthesis by cycloheximide, H-7 still showed a full effect on the increase in LPL activity. A slight but significant increase in LPL activity in the fat pads was observed with inhibitors of cyclic nucleotide-dependent protein kinase. H-7, therefore, may increase LPL activity through processes other than the direct activation of the LPL molecule, or the stimulation of LPL molecule synthesis; probably through a decrease in the activity of protein kinases, especially protein kinase C.