Myosin light chain kinase (MLCK) is a ubiquitous Ca2+/calmodulin (CaM)-activated kinase found in smooth, cardiac, and skeletal muscle as well as in mammalian nonmuscle cells.
Myosin light chain kinase (MLCK) is a regulatory protein forsmooth muscle contraction, which acts by phosphorylating 20-kDamyosin light chain (MLC20) to activate the myosin ATPase activity.Myosin light chain kinase (MLCK) of smooth muscle hasbeen puried as an enzyme that phosphorylates 20-kDa lightchain of smoothmuscle myosin (MLC20).
Analysis of the cross talk between Ras-ERK and PI3K-AKT signaling pathways reveals integrin β1, myosin light chain kinase (MLCK) and myosin IIA are required for the activation of PI3K-AKT following inhibition of the Ras-ERK pathway. Integrin β1, MLCK, and myosin IIA are factors in the development of resistance to MEK inhibitors.
Myosin light chain kinase (MLCK) phosphorylates the regulatory light chain (RLC) of myosin producing increases in force development during skeletal muscle contraction.
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A highly specific myosin II ATPase inhibitor; inhibits the Ca2+-stimulated S1 ATPase, and reversibly blocked gliding motility; inhibits isometric Ca2+-activated tension with IC50 of 3 uM in glycerol-extracted fibres from rabbit psoas muscle; specific and no activity for platelet myosin II.
Myokinasib is a mixed-type, selective inhibitor of Myosin Light Chain Kinase 1 (MLCK1) with IC50 of 7.9 uM, can bind to the free enzyme and the enzyme-substrate complex; Myokinasib inhibits only two additional kinases PLK2/3 with IC50 of 10.3/6.7 uM in a panel of 25 kinases, does not bind to the Polo-box domain of PLK2 and PLK3; impairs cytokinesis, induces formation of multinucleated cells, and reduces phosphorylated myosin II light chain abundance on stress fibers, reduces phospho-S19-MLC protein levels in cells.
Mavacamten (SAR-439152, MYK-461) is a small molecule that reduces contractility by decreasing the ATPase activity of the cardiac myosin heavy chain; inhibits α and β isoforms of cardiac myosin with similar activity (IC50=0.3 uM); suppresses the development of ventricular hypertrophy, cardiomyocyte disarray, and myocardial fibrosis and attenuates hypertrophic and profibrotic gene expression in mice harboring heterozygous human mutations in the myosin heavy chain.
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