Table 2.

IC₅₀ or Ki values of pharmacological inhibitors on MLCK activity

Pharmacological inhibitor	Target	IC50 or Ki (μM)
Wortmannin	acts at or near the catalytic domain of MLCK in a noncompetitive and irreversible manner; far more potent inhibitor of PI3K of Class 1 and Class 2132,150	IC50: 1.9
AV25	targets the auto-inhibitory site of MLCK.51	IC50: 0.2
MLCK(11-19)amide	binds to the substrate site of MLCK.129	Ki: 10
KT5926	targets the ATP-binding site of MLCK in a competitive mode and the substrate site of MLCK in a noncompetitive manner; far more potent inhibitor of CaMKII.151,152	Ki: 0.0044 - 0.018
K-252a	targets the ATP-binding site of MLCK; far more potent inhibitor of CaMKII.152,153	Ki: 0.0018 - 0.020
MS-347a	binds to the catalytic domain of MLCK in an irreversible manner.130	IC50: 9.2
ML-9	targets the ATP-binding site of MLCK.101,152	Ki: 3.9 IC50 (on NA-evoked Icat): 2
ML-7	targets the ATP-binding site of MLCK.101,152	Ki: 0.3 IC50 (on NA-evoked Icat): 0.8

IC₅₀ and Ki values with respect to MLCK activity, except for ML-7 and ML-9 where the IC₅₀ values were obtained on noradrenaline (NA)-induced cationic current (Icat).