Myosin Inhibitor

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.

MT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (K_i,NMIIA = 2.7 μM) and IIB (EC₅₀ = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma.

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.

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

Myoferlin inhibitor 1 is a compound that exhibits reversible, concentration-dependent binding to the myoferlin MYOF-C2D protein, with a K_D of 0.094 μM. Myoferlin inhibitor 1 shows potent anti-invasion and anti-migration activities against different pancreatic cancer cells. Myoferlin inhibitor 1 inhibits pancreatic cancer metastasis through reversing mesenchymal transition (EMT), inhibiting the secretions of MMP1 and MMP2 and blocking the receptor tyrosine kinases. Myoferlin inhibitor 1 displays effective antimetastatic activities in pancreatic cancer in vitro and in vivo. Myoferlin inhibitor 1 can be used in research on preventing pancreatic cancer metastasis.

(R)-MPH-220 is the R isomer of MPH-220 (HY-148516). 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.

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

LK-1 is a humanized antibody expressed in CHO that targets S100A4. LK-1 carries a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for LK-1 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

JB061 is a nonmuscle myosin inhibitor with IC₅₀s of 4.4 μM (Cardiac muscle myosin), 9.1 μM (Skeletal muscle myosin), and >100 μM (Smooth muscle myosin II), respectively. JB061 poorly decreases ATPase activity (IC₅₀>200 μM). JB061 shows cytotoxicity against COS-7 cells with an IC₅₀ value of 39 μM.

DN-F01 has a strong inhibitory calcium-dependent effect on cardiac myofibrillar ATPase activity with an IC₅₀ value of 11 ± 4 nmol/L.

Phenamacril (Standard) is the analytical standard of Phenamacril. This product is intended for research and analytical applications. Phenamacril (JS399-19) inhibits activity of myosin I non-competitively with an IC50 of 360 nM through suppression of the ATPase activity, exhibits therefore an antifungal efficacy towards Fusarium species.

Myosin-IN-2 (Example 16) is a Myosin ATPase inhibitor with a IC₅₀ of 1.06  μM. Myosin-IN-2 can be used for heart diseases like hypertrophic cardiomyopathy (HCM) research.

Myosin-IN-1 (compound F10) is a Myosin inhibitor that specifically targets cardiac myosin. Myosin-IN-1 stabilizes the biochemical and structural closed state of the cardiac myosin motor domain and reduces myocardial force production and calcium sensitivity in vitro. Myosin-IN-1 acts as a negative inotropic agent in isolated Langendroff-perfused rat hearts, reducing stress in isolated myofilaments and left ventricular pressure development. Myosin-IN-1 can be used in heart failure research.

(S)-3'-Hydroxy blebbistatin is a myosin II inhibitor and is more water-soluble than Blebbistatin.

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