MYLPF Inhibitors
Chemical inhibitors of myosin light chain phosphatase (MYLPF) can effectively regulate the activity of this protein through various molecular mechanisms. Bisindolylmaleimide I and Chelerythrine are both potent inhibitors of protein kinase C (PKC), which is essential for the phosphorylation of myosin light chains, a necessary step for MYLPF to exert its effects. By blocking PKC, these inhibitors lead to a decrease in the phosphorylation and consequent activation of myosin, thus reducing MYLPF's ability to act on these proteins. Similarly, Gö 6976, by selectively inhibiting specific isoforms of PKC, also contributes to a decline in myosin light chain phosphorylation, resulting in decreased activity of MYLPF. Moreover, Calyculin A disrupts the function of MYLPF by a different route; it inhibits protein phosphatases PP1 and PP2A, which are responsible for the dephosphorylation of myosin light chains, thereby preventing MYLPF from activating these molecular targets.
Further modulation of MYLPF activity is achieved through the inhibition of kinases that regulate the phosphorylation state of proteins that interact with MYLPF. Y-27632 and HA-1077 (Fasudil) both target Rho-associated protein kinase (ROCK), which phosphorylates and activates myosin light chain phosphatase, leading to increased myosin light chain phosphorylation. By inhibiting ROCK, these substances indirectly reduce MYLPF activity. H-1152 is a more potent inhibitor in this category, operating on the same pathway to reduce MYLPF activity. ML-7 and ML-9, on the other hand, inhibit myosin light chain kinase (MLCK), which phosphorylates myosin light chains directly, and their inhibition results in decreased phosphorylation by MLCK and thereby reduced MYLPF activity. KT-5823 impedes the function of protein kinase G (PKG), which also plays a role in the phosphorylation of the myosin-binding subunit of MYLPF, leading to a decrease in the activity of MYLPF. Lastly, W-7 and KN-93 target the calcium-calmodulin pathway, with W-7 acting as a calmodulin antagonist and KN-93 specifically inhibiting calcium/calmodulin-dependent protein kinase II (CaMKII), culminating in a reduced phosphorylation of myosin light chains which in turn diminishes the activity of MYLPF.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a potent and selective inhibitor of protein kinase C (PKC), a family of kinases that MYLPF, a myosin light chain phosphatase target subunit, is dependent on for phosphorylation which activates the myosin light chains. Inhibition of PKC leads to decreased phosphorylation of the myosin light chains, thereby reducing MYLPF activity. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
Y-27632 selectively inhibits ROCK (Rho-associated protein kinase), which phosphorylates and activates myosin light chain phosphatase, ultimately leading to increased myosin light chain phosphorylation. By inhibiting ROCK, Y-27632 indirectly reduces MYLPF activity by preventing this phosphorylation. | ||||||
ML-7 hydrochloride | 110448-33-4 | sc-200557 sc-200557A | 10 mg 50 mg | $89.00 $262.00 | 13 | |
ML-7 is an inhibitor of myosin light chain kinase (MLCK), which phosphorylates myosin light chains. By inhibiting MLCK, ML-7 decreases the phosphorylation and activation of myosin, thus indirectly diminishing MYLPF activity. | ||||||
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 is another inhibitor of myosin light chain kinase (MLCK). By inhibiting MLCK, ML-9 leads to reduced phosphorylation of myosin light chains and subsequently decreased activity of MYLPF. | ||||||
Chelerythrine | 34316-15-9 | sc-507380 | 100 mg | $540.00 | ||
Chelerythrine is a selective inhibitor of protein kinase C (PKC). It diminishes PKC activity, which is necessary for the phosphorylation of myosin light chains, thereby indirectly inhibiting MYLPF activity. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $223.00 | 8 | |
Gö 6976 is a potent inhibitor of certain PKC isoforms. It inhibits PKC-mediated phosphorylation of substrates, leading to diminished myosin light chain phosphorylation and indirectly decreasing MYLPF 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 ROCK inhibitor than Y-27632. It prevents the phosphorylation of myosin light chain phosphatase target subunit 1 (MYPT1) and thereby decreases the activity of MYLPF. | ||||||
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 calcium-calmodulin-dependent protein kinase (CaMK) which is involved in the phosphorylation of myosin light chains. Inhibition of this pathway can indirectly lead to reduced MYLPF activity. | ||||||
KN-93 | 139298-40-1 | sc-202199 | 1 mg | $178.00 | 25 | |
KN-93 is a specific inhibitor of calcium/calmodulin-dependent protein kinase II (CaMKII). By inhibiting CaMKII, KN-93 indirectly decreases the phosphorylation of myosin light chains, thus inhibiting MYLPF activity. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A sc-24000B sc-24000C | 10 µg 100 µg 500 µg 1 mg | $160.00 $750.00 $1400.00 $3000.00 | 59 | |
Calyculin A is an inhibitor of protein phosphatases PP1 and PP2A. By inhibiting these phosphatases, it prevents dephosphorylation of myosin light chains, which would otherwise be necessary for the activation of MYLPF. | ||||||