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KN-62, 1-[N,O-bis-(5-isoquinolinesulphonyl)-N-methyl-L-tyrosy]-4-phenylpiperazine is a highly selective inhibitor of the calcium dependent calmodulin protein kinase II (CAMKII), which binds to the calmodulin binding site of CAMKII and consequently does not inhibit other classes of calmodulin-sensitive kinases. In previous studies, KN-62 exhibits inhibitory effects on the regulated secretion of insulin by hetero-junction with intrinsic thin-layer (HIT) cells and the cholecystokinin secretion from stanniocalcin-1 (STC-1) enteroendocrine cells due to a block of Ca2+ influx through L-type Ca2+ channels in the olasma membrane. It also inhibits both insulin- and hypoxia-stimulated glucose transport activity by 46% and 40% respectively in skeletal muscle.

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