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.

Myosin-IN-4 (Compound 3), a pyridine-2,4-dione derivative, is a myocardial myosin inhibitor. Myosin-IN-4 has a strong inhibitory activity against cardiac myosin ATPase with an IC₅₀ value of 0.73 μM. Myosin-IN-4 exert a negative inotropic effect by inhibiting myocardial contraction. Myosin-IN-4 can be used for the research on cardiovascular diseases related to cardiac myosin.

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.

(+)-Blebbistatin is the inactive enantiomer of (–)-Blebbistatin. (–)-Blebbistatin is a selective inhibitor of myosin II ATPase.

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.