Myosin Inhibitor

Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function. Blebbistatin blocks cell migration.

(-)-Blebbistatin is a selective inhibitor of the ATPase activity of non-muscle myosin II.

W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca²⁺-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC₅₀ values of 28 μM and 51 μM, respectively. W-7 hydrochloride induces apoptosis and has antitumor and vascular relaxing activity. W-7 hydrochloride is a blocker of Kv4.3 and can be used for research of arrhythmias.

(+)-Blebbistatin is the inactive enantiomer of (-)-Blebbistatin (HY-13441). (-)-Blebbistatin is a selective inhibitor of non-muscle myosin II ATPase activity.

Aficamten (CK-274) is a potent cardiac myosin inhibitor with an IC₅₀ of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM).

para-Nitroblebbistatin is a derivative of Blebbistatin (HY-13813) and an inhibitor of myosin II. para-Nitroblebbistatin is photostable, non-cytotoxic, and non-phototoxic. para-Nitroblebbistatin can serve as an ideal substitute for Blebbistatin (HY-13813) to study the role of myosin II in physiology, development, and cell biology.

Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca²⁺ release.

Sevasemten is an orally active, selective allosteric inhibitor of skeletal muscle myosin that protects skeletal muscle from contraction-induced injury. Sevasemten decreases muscle damage biomarkers and fibrosis while increasing muscle strength and activity in in Duchenne muscular dystrophy disease models.

ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with K_i values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.

BTS (N-Benzyl-p-toluenesulfonamide) is a potent and selective inhibitor of skeletal muscle myosin II subfragment 1 (S1) ATPase activity, with an IC₅₀s of ~5 µM for actin- and Ca²⁺-stimulated myosin S1 ATPase. BTS specifically inhibits the contraction of fast skeletal muscle fibers.

Para-aminoblebbistatin is the inhibitor for myosin II. Para-aminoblebbistatin inhibits the ATPase activity of myosin II, thereby blocking the formation and contraction of the actin-myosin network. Para-aminoblebbistatin is a non-fluorescent and photostable Blebbistatin (HY-13813) derivative.

MPH-220 is a selective and orally active inhibitor of skeletal muscle myosin-2. MPH-220 enables muscle relaxation. MPH-220 is anti-spastic agent that can be used in the research of spasticity and muscle stiffness.

Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC₅₀s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC₅₀ of 0.1 to 0.2 μM for TGF-β.

NU074381b (compound 5b) is a potent S100A4 inhibitor. NU074381b inhibits S100A4-NMII complex formation with an IC₅₀ value of 0.48 µM. NU074381b inhibits cell proliferation and migration.

Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a K_i of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex.

MT-228 (BPN-0026709) is a selective and blood-brain barrier permeable non-muscle myosin II inhibitor. MT-228 markedly improves tolerability by selectively targeting NMIIB (K_I = 1.5 μM) over CMII (K_I = 17 μM), and the sequence of SmMll MD is 83.6% identical to that of NMllB. MT-228 shows long-lasting efficacy in animal models of stimulant use disorder.

MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder.

AX-202 is a humanized IgG4 monoclonal antibody targeting S100A4. AX-202 neutralizes the activity of S100A4. AX-202 effectively reverses established fibrosis and reduces inflammation and fibrosis-related biomarkers in a mouse model of skin fibrosis. AX-202 is applicable for the research of fibrotic and inflammatory diseases.

ATM-3507 is a potent tropomyosin inhibitor with IC₅₀s from 3.83-6.84 μM in human melanoma cell lines.

Delocamten is an orally active, selective Cardiac Myosin inhibitor with an IC₅₀ of approximately 1.11 μM. Delocamten directly modulates myosin complexes, inhibits excessive myocardial contraction, and improves diastolic function. Delocamten can be used in studies of hypertrophic cardiomyopathy (HCM), left ventricular hypertrophy, and diastolic dysfunction.