Mylc2b Inhibitors
Chemical inhibitors of Mylc2b disrupt its normal function in muscle contraction through various molecular mechanisms. W-7 Hydrochloride and ML-9 are two such inhibitors that directly target the phosphorylation process essential for Mylc2b activation. W-7 Hydrochloride inhibits the calmodulin-dependent kinase, a pivotal enzyme in the phosphorylation of Mylc2b, thus preventing its activation and subsequent muscle contraction. Similarly, ML-9 acts by specifically inhibiting myosin light chain kinase (MLCK), the direct kinase responsible for phosphorylating Mylc2b. By blocking MLCK, ML-9 ensures that Mylc2b remains in an unphosphorylated, inactive state, which is unable to interact with actin filaments and generate muscle contraction.
Other chemical inhibitors, like KN-93 Phosphate, Y-27632, and H-1152 dihydrochloride, indirectly affect the phosphorylation state of Mylc2b. KN-93 Phosphate targets calcium/calmodulin-dependent protein kinase II (CaMKII), which has downstream effects on Mylc2b phosphorylation. By inhibiting CaMKII, KN-93 Phosphate indirectly prevents Mylc2b activation. Y-27632 and H-1152 dihydrochloride both inhibit Rho-associated protein kinase (ROCK), which is involved in phosphorylating and inhibiting the myosin phosphatase targeting subunit (MYPT1). This inhibition increases the activity of MYPT1, leading to enhanced dephosphorylation of Mylc2b, thereby reducing its ability to promote muscle contraction. Additionally, Blebbistatin interferes with muscle contraction by selectively inhibiting the ATPase activity of the myosin II motor domain, which is necessary for Mylc2b to exert its effects. Gö 6976 and Chelerythrine Chloride work by inhibiting protein kinase C (PKC), which phosphorylates various substrates that modulate Mylc2b activity, while HA-1077, another ROCK inhibitor, further elucidates the role of ROCK in controlling Mylc2b function. Lastly, ML-7 Hydrochloride and MLCK Inhibitor Peptide 18 serve as direct inhibitors of MLCK, leading to a decrease in Mylc2b phosphorylation and muscle contraction. Staurosporine, a non-selective kinase inhibitor, broadly reduces the activity of kinases involved in Mylc2b regulation, thus broadly inhibiting its function. These inhibitors collectively elucidate the complex regulation of Mylc2b and its pivotal role in muscle contraction.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
W-7 | 61714-27-0 | sc-201501 sc-201501A sc-201501B | 50 mg 100 mg 1 g | $166.00 $306.00 $1675.00 | 18 | |
W-7 Hydrochloride directly inhibits calmodulin-dependent kinase, which is essential for Mylc2b phosphorylation. This inhibition prevents Mylc2b from achieving its active phosphorylated state, thus reducing its ability to interact with actin filaments in muscle contraction. | ||||||
ML-9 | 105637-50-1 | sc-200519 sc-200519A sc-200519B sc-200519C | 10 mg 50 mg 100 mg 250 mg | $112.00 $449.00 $673.00 $1224.00 | 2 | |
ML-9 is a kinase inhibitor that specifically targets myosin light chain kinase (MLCK), which phosphorylates Mylc2b. By inhibiting MLCK, ML-9 prevents the phosphorylation and subsequent activation of Mylc2b, leading to a decrease in muscle contraction and smooth muscle tone. | ||||||
KN-93 | 139298-40-1 | sc-202199 | 1 mg | $182.00 | 25 | |
KN-93 inhibits calcium/calmodulin-dependent protein kinase II (CaMKII). CaMKII indirectly influences the phosphorylation state of Mylc2b by modulating the kinase activity towards Mylc2b. Therefore, KN-93 Phosphate inhibits the phosphorylation and activation of Mylc2b. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
Y-27632 inhibits Rho-associated protein kinase (ROCK), which is involved in the phosphorylation of myosin phosphatase targeting subunit (MYPT1), a process that indirectly affects Mylc2b function. By inhibiting ROCK, Y-27632 prevents the inhibition of MYPT1, leading to enhanced dephosphorylation of Mylc2b and thereby reduced contractile activity. | ||||||
(±)-Blebbistatin | 674289-55-5 | sc-203532B sc-203532 sc-203532A sc-203532C sc-203532D | 5 mg 10 mg 25 mg 50 mg 100 mg | $183.00 $313.00 $464.00 $942.00 $1723.00 | 7 | |
Blebbistatin is a selective inhibitor of myosin II ATPase activity. By binding to the myosin II motor domain, it prevents Mylc2b-containing myosin from transitioning to a state capable of force generation and movement, thus inhibiting muscle contraction. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $227.00 | 8 | |
Gö 6976 is a potent inhibitor of protein kinase C (PKC), which can phosphorylate multiple substrates, including those that modulate the activity of Mylc2b. By inhibiting PKC, Gö 6976 reduces the phosphorylation of proteins that are involved in the activation of Mylc2b, leading to decreased Mylc2b-mediated muscle contraction. | ||||||
H-1152 dihydrochloride | 451462-58-1 | sc-203592 sc-203592A | 1 mg 5 mg | $104.00 $364.00 | 7 | |
H-1152 dihydrochloride is another inhibitor of Rho-associated protein kinase (ROCK), similar to Y-27632. It prevents the ROCK-mediated inhibition of myosin phosphatase activity, which in turn promotes the dephosphorylation of Mylc2b. This action results in the functional inhibition of Mylc2b, reducing its ability to promote muscle contraction. | ||||||
ML-7 hydrochloride | 110448-33-4 | sc-200557 sc-200557A | 10 mg 50 mg | $91.00 $267.00 | 13 | |
ML-7 Hydrochloride inhibits MLCK, directly reducing the phosphorylation of Mylc2b. The decrease in phosphorylated Mylc2b leads to a functional inhibition of its activity in muscle contraction processes. | ||||||
Chelerythrine chloride | 3895-92-9 | sc-3547 sc-3547A | 5 mg 25 mg | $90.00 $317.00 | 17 | |
Chelerythrine Chloride is an inhibitor of PKC. By inhibiting PKC, it reduces the phosphorylation and activation of downstream targets that regulate the activity of Mylc2b. This inhibition results in a decrease of Mylc2b's ability to facilitate muscle contraction. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine is a non-selective kinase inhibitor, which can inhibit a broad range of kinases including those directly or indirectly involved in the phosphorylation and activation of Mylc2b. By inhibiting these kinases, Staurosporine leads to reduced phosphorylation and activity of Mylc2b | ||||||