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.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H6273 |
Danicamtiv |
1970972-74-7 | Danicamtiv is a positive inotropic agent. |
H2420 |
Myokinasib |
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. |
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H2419 |
ML-9 hydrochloride |
105637-50-1 | ML-9 hydrochloride is a potent, ATP-competitive myosin light chain kinase (MLCK) inhibitor with Ki of 3.8 uM, inhibits Store-operated Ca2+ entry (SOCE) in a variety of cell lines; also inhibits PKA and PKC with Ki of 32 and 54 uM; inhibits STIM1-plasma membrane interactions and inhibits TRPC6 channels via a mechanism independent of inhibition of MLCK activity. |
H2418 |
Mavacamten |
1642288-47-8 |
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. |
H2417 |
BTS |
1576-37-0 | 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. |
H2416 |
Blebbistatin S enantiomer |
856925-71-8 | Blebbistatin S enantiomer ((S)-(-)-Blebbistatin) is the S enantiomer of blebbistatin, which is a potent and selective myosin II inhibitor with IC50 of 0.5-5 uM; inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly, inhibits pancreatic adenocarcinoma cellular invasiveness; inhibits some myosin II-independent processes and that blebbistatin inhibits other activities in the absence of myosin II. |
H2415 |
BHC |
342387-19-3 | BHC (Myosin inhibitor BHC) is a small-molecule screen of skeletal muscle myosin inhibitor that suppresses movements without affecting membrane currents; selectively blocks nerve-evoked muscle contraction without affecting neurotransmitter release. |
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