MLCKSK Inhibitors
MLCKSK inhibitors are a class of chemical compounds that selectively inhibit the activity of myosin light chain kinase (MLCK) and, to a lesser extent, spleen tyrosine kinase (Syk). MLCK is an enzyme primarily responsible for the phosphorylation of the regulatory light chain of myosin II, a process essential for modulating the interaction between myosin and actin filaments during cellular contractility and motility. By inhibiting MLCK, these inhibitors interfere with actomyosin contractility, impacting cellular processes such as migration, adhesion, and permeability. This makes MLCKSK inhibitors critical in research that aims to understand the regulation of cytoskeletal dynamics and cell morphology. Additionally, Syk is involved in signal transduction pathways within the immune response, and while MLCKSK inhibitors primarily target MLCK, their interaction with Syk provides an added layer of complexity in cellular signaling research.
The molecular structures of MLCKSK inhibitors are designed to fit into the ATP-binding site of MLCK, blocking its enzymatic function. This binding is generally ATP-competitive, preventing the transfer of a phosphate group to the myosin light chain. Due to the highly specific nature of MLCKSK inhibitors, their use extends to studies exploring the fine-tuned regulation of cellular tension, mechanotransduction, and vascular biology. The inhibition of MLCK also affects endothelial and epithelial cell barrier function, influencing studies on fluid transport across these layers. On the Syk side, its partial inhibition by these compounds allows researchers to dissect immune-related pathways, although this effect is often secondary compared to MLCK inhibition. Overall, MLCKSK inhibitors are invaluable tools for studying cytoskeletal regulation and cell signaling pathways with precision.
SEE ALSO...
Items 1 to 10 of 11 total
Display:
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
ML-7 hydrochloride | 110448-33-4 | sc-200557 sc-200557A | 10 mg 50 mg | $89.00 $262.00 | 13 | |
ML-7 is a specific inhibitor of myosin light chain kinase (MLCK). It inhibits MLCKSK by binding to the ATP-binding site of the kinase, preventing ATP from binding, which is necessary for the phosphorylation of the myosin light chain and subsequent muscle contraction. | ||||||
ML-9 | 105637-50-1 | sc-200519 sc-200519A sc-200519B sc-200519C | 10 mg 50 mg 100 mg 250 mg | $110.00 $440.00 $660.00 $1200.00 | 2 | |
ML-9, like ML-7, inhibits MLCK through competitive inhibition at the ATP-binding site. By occupying this site, ML-9 prevents ATP from initiating the phosphorylation cascade that MLCKSK catalyzes, thereby inhibiting its function. | ||||||
W-7 | 61714-27-0 | sc-201501 sc-201501A sc-201501B | 50 mg 100 mg 1 g | $163.00 $300.00 $1642.00 | 18 | |
W-7 is a calmodulin antagonist that inhibits MLCKSK by preventing calmodulin from activating the kinase. Since MLCK is dependent on calmodulin for its activity, W-7 effectively inhibits MLCKSK by disrupting this crucial protein-protein interaction. | ||||||
KN-93 | 139298-40-1 | sc-202199 | 1 mg | $178.00 | 25 | |
KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent protein kinase (CaMK), which can indirectly inhibit MLCKSK by altering calcium/calmodulin signaling pathways that would otherwise activate MLCK. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Staurosporine is a potent inhibitor of protein kinases, including MLCKSK. It inhibits the protein by binding to its ATP binding site, preventing ATP from binding and subsequent phosphorylation activity. | ||||||
H-1152 dihydrochloride | 451462-58-1 | sc-203592 sc-203592A | 1 mg 5 mg | $102.00 $357.00 | 7 | |
H-1152 is a more potent and selective inhibitor of Rho-associated protein kinase (ROCK), which is upstream of MLCK. It indirectly inhibits MLCKSK by inhibiting ROCK, which can reduce the phosphorylation levels of the myosin light chain, a substrate of MLCK. | ||||||
Chelerythrine | 34316-15-9 | sc-507380 | 100 mg | $540.00 | ||
Chelerythrine is a potent inhibitor of protein kinase C (PKC), which can indirectly inhibit MLCKSK by modulating PKC-mediated signaling pathways that may influence MLCK activity. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is another PKC inhibitor that can indirectly inhibit MLCKSK by reducing PKC's phosphorylation activity, which may have downstream effects on the kinase's function. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
Y-27632 is a selective inhibitor of ROCK, by inhibiting ROCK, it can reduce the activity of downstream targets such as MLCKSK. Since ROCK can phosphorylate and activate MLCK, inhibiting ROCK leads to decreased MLCKSK activity. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $223.00 | 8 | |
Gö 6976 is a potent inhibitor of Janus kinase 2 (JAK2) and protein kinase C (PKC), which can indirectly inhibit MLCKSK by disrupting the signaling pathways involving these kinases that could be upstream regulators of MLCK activity. | ||||||