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.

ML-7 hydrochloride is a selective and highly specific myosin light chain kinase (MLCK) inhibitor that acts as a trabecular meshwork (TM) relaxant. ML-7 hydrochloride enhances Quinocetone (HY-123581)-induced phosphorylation of ERK, p38 MAPK and JNK, attenuates Akt activation, and promotes apoptosis of hepatocellular carcinoma cells. ML-7 hydrochloride reduces Th2 cytokine secretion by inhibiting MLCK, while alleviating smooth muscle hyperplasia and collagen deposition. As a non-antibiotic adjuvant, ML-7 hydrochloride restores the sensitivity of drug-resistant bacteria to Tigecycline (HY-B0117). ML-7 hydrochloride can be used in research related to glaucoma, hepatocellular carcinoma, asthma, and Klebsiella pneumoniae infection.

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-5 (example 3) is a selective cardiac myosin inhibitor with an IC₅₀ of 1.5 μM. Myosin-IN-5 shows much less effective in inhibiting skeletal myofibril activity (IC₅₀ of 43.4 μM). Myosin-IN-5 can be used for the study of hypertrophic cardiomyopathy (HCM) and cardiac diseases.

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.

MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC₅₀ of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.

HJ445A is an orally active myoferlin (MYOF) inhibitor with a K_d value of 0.17 μM against human targets. HJ445A directly binds to the MYOF-C2D domain to stabilize the MYOF protein, thereby regulating vesicle trafficking, cell proliferation, colony formation, migration and apoptosis processes in cancer cells, and exhibits anti-tumor efficacy. HJ445A can be used in gastric cancer-related research.

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.

MT-125 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 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma.

HA-100 is a potent protein kinase inhibitor, with IC₅₀s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.

Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC₅₀ of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy.

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