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Myosin inhibitors and activators act on the actin-based motor proteins of muscle and non-muscle cells. Myosins hydrolyze adenosine triphosphate (ATP) and convert that chemical energy into movement along actin filaments. Blebbistatin was introduced in 2003 as a selective inhibitor of non-muscle myosin II and is used to study cytokinesis and cortical tension. The catalogue lists it as (-)-Blebbistcitin together with para-Nitroblebbistatin, a photostable analog suited to imaging experiments. Omecamtiv mecarbil works in the opposite direction and accelerates the cardiac myosin ATPase cycle. ML 7 hydrochloride and ML-9 hydrochloride act upstream on myosin light chain kinase, as does the neighboring MLCK category.
Synonyms: (S)-Blebbistatin
Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
Synonyms: ML-7 HCl
ML 7 hydrochloride is a selective inhibitor of myosin light chain kinase (MLCK).
A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).
Synonyms: BE-34776
MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.
Synonyms: ML9
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 Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
para-Nitroblebbistatin is a non-cytotoxic, photostable, fluorescent and specific Myosin II inhibitor, usd in the study of the specific role of myosin II in physiological, developmental, and cell biological studies.
ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.
Synonyms: N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine
BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility.
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain).
2,3-Butanedione monoxime (BDM, Diacetyl monoxime, Diacetylmonoxime) is the well-characterized, low-affinity, non-competitive inhibitor of skeletal muscle myosin-II and inhibits skeletal and cardiac muscle contraction.
Synonyms: (±)-Blebbistatin
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.
Myosin-IN-5 is a selective inhibitor of cardiac myosin, exhibiting an IC50 value of 1.5 μM. This compound demonstrates significantly reduced efficacy against skeletal myofibril activity, with an IC50 of 43.4 μM. Myosin-IN-5 is primarily utilized in research pertaining to hypertrophic cardiomyopathy (HCM) and other cardiac disorders, offering valuable insights into the mechanisms of cardiac muscle function and disease pathophysiology.
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Synonyms: CK-274; CK-3773274
Aficamten (CK-274) is a potent inhibitor of cardiac myosin, exhibiting an IC50 of 1.4 μM. It is primarily utilized in research focused on hypertrophic cardiomyopathy (HCM), providing valuable insights into cardiac muscle function and potential therapeutic strategies. Aficamten's ability to modulate myosin activity makes it a critical tool for exploring the molecular mechanisms underlying heart muscle disorders.
Synonyms: EDG-5506
Sevasemten is a selective allosteric inhibitor targeting skeletal muscle myosin. It demonstrates significant protective effects against contraction-induced injury in skeletal muscle, contributing to a decrease in muscle damage biomarkers and fibrosis. Additionally, sevasemten enhances muscle strength and activity in models of Duchenne muscular dystrophy, making it a valuable tool for research applications related to muscle degeneration and recovery.
MPH-220 is a selective and orally active inhibitor of skeletal muscle myosin-2. This compound promotes muscle relaxation and serves as an effective anti-spastic agent. MPH-220 is primarily utilized in research exploring spasticity and muscle stiffness, providing a valuable tool for understanding and potentially treating related disorders.
Para-aminoblebbistatin is a selective inhibitor of myosin II, acting primarily by inhibiting its ATPase activity. This inhibition effectively disrupts the formation and contraction of the actin-myosin network, making it a valuable tool for studying muscle contraction and cellular motility. As a non-fluorescent and photostable derivative of Blebbistatin, it offers reliable performance in various biological research applications.
Synonyms: d-Blebbistatin
(+)-Blebbistatin is a myosin II ATPase inhibitor that selectively targets myosin motor proteins. It is utilized in research to study cellular processes involving myosin, including muscle contraction, cell motility, and cytokinesis. Its inhibitory effects on myosin activity make it a valuable tool for investigating the roles of myosin in various biological systems.
Myosin V-IN-1 is a selective inhibitor of Myosin V, exhibiting a Ki value of 6 μM. This compound effectively slows the actin-activated myosin V ATPase activity by specifically blocking ADP release from the actomyosin complex. Myosin V-IN-1 is valuable for research into muscle contraction mechanisms and actin-based motility.
Synonyms: CK-4021586; CK-586
Ulacamten is a selective cardiac myosin inhibitor that targets the double-headed cardiac heavy meromyosin (HMM) ATPase, exhibiting an EC50 of 2.9 μM. This compound effectively modulates cardiac myosin activity, leading to reduced myocardial contractility and alleviation of left ventricular outflow tract obstruction. Ulacamten has demonstrated the ability to increase left ventricular short-axis systolic internal diameter and inhibit obstruction exacerbated by dobutamine, while minimally impacting left ventricular systolic function and calcium transients. Its safety and tolerability have been confirmed in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy, making it a valuable tool for cardiac research applications.
Delocamten is a selective inhibitor of cardiac myosin with an IC50 of 1.1 μM. It inhibits myosin-driven muscle contraction, making it a valuable tool for studying hypertrophic cardiomyopathy, left ventricular hypertrophy, and diastolic dysfunction. Delocamten is critical for research into the molecular mechanisms underlying cardiac muscle disorders and therapeutic interventions targeting these conditions.
Myosin-IN-1 is a selective myosin inhibitor that specifically targets cardiac myosin. By stabilizing the closed state of the cardiac myosin motor domain, it effectively reduces myocardial force production and calcium sensitivity in vitro. Its function as a negative inotropic agent has been demonstrated in isolated Langendorff-perfused rat hearts, where it decreases stress in isolated myofilaments and left ventricular pressure development. This compound is suitable for applications in heart failure research, making it a valuable tool for investigating cardiac physiology and pathophysiology.
(S)-3'-Hydroxy blebbistatin is a selective inhibitor of myosin II, offering enhanced water solubility compared to its parent compound, Blebbistatin. This reagent effectively disrupts myosin II-driven cellular processes, making it a valuable tool for investigating cytoskeletal dynamics and cellular motility. Its potency and improved solubility facilitate a range of applications in cell biology and biophysics research.
JB062 is a selective nonmuscle myosin inhibitor that exhibits IC50 values of 1.6 μM for skeletal muscle myosin, 5.4 μM for cardiac muscle myosin, and greater than 100 μM for smooth muscle myosin II. This compound demonstrates cytotoxic effects on human cancer cells while sparing normal cells, making it a valuable tool in cancer research. JB062 is suitable for investigations related to muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.
(S)-3'-Aminoblebbistatin is a potent inhibitor of myosin II, demonstrating an IC50 value of 14.1 µM. This compound serves as a valuable tool for studying the role of myosin II in cellular processes such as motility, division, and contraction. Its ability to specifically target myosin II makes it an essential reagent for researchers investigating muscle physiology, cell migration, and related mechanistic pathways.
JB002 is a selective inhibitor of myosin II, exhibiting an IC50 of ≤10 μM. This compound is significant for studying various conditions such as muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy. JB002 aids in understanding the role of myosin II in muscle dynamics and associated pathological states, providing a valuable tool for biomedical research.
