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MLCK inhibitors block myosin light chain kinase, the enzyme that switches on smooth muscle contraction. Myosin light chain kinase (MLCK) is a calcium and calmodulin-dependent kinase that phosphorylates the regulatory light chain of myosin II. This step starts actomyosin contraction in smooth muscle and also regulates endothelial barrier function and cell migration. The naphthalenesulfonyl compounds ML-7 and ML-9 were described in 1987 as selective inhibitors of smooth muscle MLCK. ML 7 hydrochloride, ML-9 hydrochloride and MS-444 are the MLCK inhibitors listed here. BTS acts further downstream, inhibiting skeletal muscle myosin II ATPase activity. Broader kinase tools such as (E)-KN-93 phosphate and GF 109203X also appear, while motor protein inhibitors are covered under Myosin.
Synonyms: ML-7 HCl
ML 7 hydrochloride is a selective inhibitor of myosin light chain kinase (MLCK).
A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).
Synonyms: BE-34776
MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.
Synonyms: ML9
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
Synonyms: N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine
BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility.
