Myosin V-IN-1 is a potent and selective inhibitor of Myosin V with a Ki value of 6 μM.Myosin V-IN-1 inhibits actin V and slows down actin-activated myosin V ATPase by selectively inhibiting the release of ADP from the actinoglobulin complex.

Myosin light chain kinase fragment 11-19 amide (MLCK(11-19) amide) serves both as a substrate-specific peptide inhibitor of MLCK and as an inhibitor of hypotonicity-induced Ca2+ entry. This compound has applications in the research of human cervical cancer [1] [2].

Myosin H Chain Fragment, mouse acetate salt, a segment of the α-Myosin heavy chain peptide, is instrumental in developing the experimental autoimmune myocarditis (EAM) mouse model [1] [2].

Myosin H Chain Fragment, mouse, is a segment of the α-Myosin heavy chain peptide and serves as an inducer of experimental autoimmune myocarditis (EAM) in mouse models [1] [2].

Blebbistatin ((±)-Blebbistatin) is a selective non-muscle myosin II (NMII) inhibitor. It promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing. Furthermore it preserves cell junctional integrity and barrier function.Blebbistatin is an inhibitor of MYH9.

JB062 is a chemical compound acting as a nonmuscle myosin inhibitor, exhibiting IC50 values of 1.6, 5.4, and >100 μM against skeletal muscle myosin, cardiac muscle myosin, and smooth muscle myosin II, respectively. It selectively exhibits cytotoxicity towards human cancer cells without affecting normal cells. The compound is applicable in research fields concerning muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

Phenamacril (JS39919) is acyanoacrylate fungicide, has powerful inhibition against Fusarium species, especially to Fusarium graminearum. Phenamacril is a specific Fusarium myosin I inhibitor.

Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits the localization of phosphorylated MRLC (Myosin Regulatory Light Chain) and acts by specifically inhibiting Rho kinase activity.

MLCK inhibitor peptide 18 acetate is a selective competitive inhibitor of myosin light chain kinase (IC50 = 50 nM). Displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. Cell permeable.

MS-444 suppresses the activity of purified smooth muscle myosin light chain kinase (MLCK) (IC50: 10 μM).

para-Nitroblebbistatin (p-Nitroblebbistatin) is a non-cytotoxic, fluorescent, photostable and specific Myosin II inhibitor. para-Nitroblebbistatin can be used in the study of the special role of myosin II in developmental, physiological,, and cell biological studies.

CCG-257081 (MRTF/SRF-IN-1) is an inhibitor of cardiac myosin-related transcription factor and serum response factor (MRTF/SRF) that acts by inhibiting the Rho/MRTF/SRF pathway.CCG-257081 has shown efficacy in preventing bleomycin-induced fibrosis in several mouse models. CCG-257081 can be used in cancer prevention and fibrosis research.

ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.

HA-100 is an inhibitor of protein kinase

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

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM.

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Selective competitive inhibitor of myosin light chain kinase (IC50 = 50 nM). Displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. Cell permeable.

Calmodulin Binding Peptide 1, a potent CaM-binding peptide with picomolar (pM) affinity, originates from smooth muscle myosin light-chain kinase (MLCK peptide). It effectively blocks inositol trisphosphate (IP3)-induced calcium (Ca2+) release [1].

Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin/phospho-myosin II co-aggregates by stimulation of the RhoA/ROCK pathway and inhibition of LIM-Kinase.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

Sevasemten is an allosteric inhibitor that targets skeletal muscle myosin. It displays selectivity in its inhibition, demonstrated by IC50 values of ≤10 μM for skeletal muscle myosin and >100 μM for cardiac myosin, respectively.

(3S,4R)-PF-6683324 is a pro-myosin-related kinase (Trk) inhibitor that has shown research potential for pain and cancer.

SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR-33805.

Diazobenzenesulfonic acid is a whiter or reddish crystalline acid derivative of sulfanilic acid. It is a desensitizer (inhibitor) of allosteric effect for myosin ATPase 13.

Omecamtiv mecarbil (CK-1827452) has been used in trials studying the treatment and basic science of Heart Failure, Echocardiogram, Pharmacokinetics, Chronic Heart Failure, and History of Chronic Heart Failure, among others.

Mavacamten-d6 is a deuterated compound of Mavacamten. Mavacamten has a CAS number of 1642288-47-8. MYK-461 is an orally bioavailable inhibitor of cardiac myosin ATPase,( IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively)

2,3-Butanedione 2-Monoxime (Diacetyl monoxime) is an inhibitor of skeletal and cardiac muscle contraction.

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

Pentabromopseudilin (PBrP), a marine antibiotic derived from Pseudomonas bromoutilis and Alteromonas luteoviolaceus, demonstrates antimicrobial, antitumor, and phytotoxic properties. It acts as a reversible, allosteric inhibitor of myosin Va (MyoVa) and robustly inhibits transforming growth factor-β (TGF-β) activity. PBrP is utilized in researching fibrotic diseases and cancer [1].

MPH-220 is a selective, orally active skeletal muscle myosin-2 inhibitor that facilitates muscle relaxation. As an anti-spastic agent, it holds potential for research into spasticity and muscle stiffness.

Pentachloropseudilin (PClP) is a reversible variant 1 myosin inhibitor with antimicrobial activity that inhibits Myo1s and class 5 myosins.Pentachloropseudilin inhibits growth factor-beta (TGF-β), which blocks host cell invasion by Trypanosoma cruzi.

W-7 hydrochloride (W-7 HCl), a calmodulin antagonist, inhibits Ca2+-calmodulin-dependent myosin light chain kinase and phosphodiesterase, W-7 hydrochloride induces apoptosis and has antitumor activity.

Ritodrine hydrochloride (NSC 291565) binds to and activates beta-2 adrenergic receptors of myometrial cells in the uterus, which decreases the intensity and frequency of uterine contractions. Ritodrine hydrochloride (NSC 291565) is a phenethylamine derivative with tocolytic activity. Specifically, Ritodrine hydrochloride (NSC 291565) probably activates adenyl cyclase, thereby increasing production of cyclic adenosine monophosphate (cAMP), which in turn enhances the efflux of calcium from vascular smooth muscle cells. A lack of intracellular calcium prevents uterine myometrial contractions. In addition, this agent may directly inactivate myosin light chain kinase, a critical enzyme necessary for the initiation of muscle contractions.

BTS (N-Tosylbenzylamine) is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 : 5 μM) .

JB002, a myosin II inhibitor, exhibits potent activity with an IC50 of ≤10 μM. It holds potential for research applications in muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1]. A-3 hydrochloride against P

Aficamten is a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy.

Danicamtiv (MYK-491) is an inotropic agent and it also is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.

(S)-3'-amino Blebbistatin, retaining the active stereochemistry of the less stable and more phototoxic (–)-blebbistatin, serves as a refined selective cell-permeable inhibitor of non-muscle myosin II ATPases. This compound efficaciously inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across several species with IC50s ranging from 0.5-5 µM, and exhibits minimal inhibition against smooth muscle myosin (IC50= 80 µM). Its primary functions include obstructing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. (S)-3'-amino Blebbistatin overcomes (–)-blebbistatin’s limitation of rapid degradation under blue light (450-490 nm) exposure, which generates cytotoxic intermediates, thus posing a challenge for fluorescent live cell imaging applications. The introduction of a 3’-amino group to its structure notably reduces fluorescence while maintaining (–)-blebbistatin’s activity, making it a superior alternative for research purposes.

JB061 is a nonmuscle myosin inhibitor, demonstrating selective inhibitory activity with IC50 values of 4.4 μM (Cardiac muscle myosin), 9.1 μM (Skeletal muscle myosin), and >100 μM (Smooth muscle myosin II). It exhibits limited efficacy in reducing ATPase activity, with an IC50 exceeding 200 μM. Furthermore, JB061 displays cytotoxic effects on COS-7 cells, evidenced by an IC50 value of 39 μM.

ML-9 (free base) suppresses MLCK, PKA, and PKC activity (Ki: 4, 32, and 54 μM, respectively). ML-9 (free base) is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) acti

Myoferlin inhibitor 1 is a novel anti-metastatic agent against pancreatic cancer that acts on myosin.

YQ456 is a novel small molecule inhibitor of myosin that binds myosin with high affinity (KD: 37 nM) and is highly resistant to invasion (IC50: 110 nM).

Hydralazine hydrochloride (Apresoline) is the hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release and interferes with smooth muscle cell calcium influx, resulting in arterial vasodilatation. This agent also inhibits the phosphorylation of myosin protein and chelation of trace metals required for smooth muscle contraction, resulting in an increase in heart rate, stroke volume, and cardiac output. In addition to its cardiovascular effects, hydralazine inhibits DNA methyltransferase, which may result in inhibition of DNA methylation in tumor cells.

3,5-Diiodothyropropionic acid (C082182) is a thyroid hormone analog. It induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (Ka: 2.40/M and 4.06/M for TRα1 and TRβ1).

(S)-nitro-Blebbistatin is a more stable form of (-)-blebbistatin , which is a selective cell-permeable inhibitor of non-muscle myosin II ATPases. (-)-Blebbistatin rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM). Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications. The addition of a nitro group stabilizes the molecule to circumvent its degradation by prolonged blue light exposure. (S)-nitro-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer.

Mavacamten (MYK-461) is an orally bioavailable inhibitor of cardiac myosin ATPase,( IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively)

MS 347a is a myosin light chain kinase (MLCK) inhibitor; an epoxide analog of sydowinin B (MS-347b).

Paltimatrectinib (PBI-200) is a potent tyrosine kinase inhibitor with anticancer activity that inhibits myosin-related kinase A (TrkA).Paltimatrectinib is used in the study of bladder, breast and colorectal cancers.