myosin

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.

ATM-3507 is a protomyosin inhibitor with anticancer activity that inhibits human melanoma and can be used to study ovarian cancer.

para-Nitroblebbistatin is a non-cytotoxic, non-fluorescent, photostable, and specific inhibitor of myosin II. para-Nitroblebbistatin can be used to study the specific roles of myosin II in physiology, development, and cell biology.

MS-444 (BE-34776) is a smooth muscle myosin light chain kinase (MLCK) and HuR inhibitor with antitumor activity for triple-negative breast and colorectal cancer.

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

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.

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.

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.

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.

Blebbistatin ((±)-Blebbistatin) is a non-muscle myosin II (NMII)-selective and non-muscle myosin heavy chain 9 (MYH9)-specific inhibitor that promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, while preserving the integrity of cell junctions and barrier function.

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

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

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.

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.

(-)-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.

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.

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.

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.

HA-100 is an inhibitor of protein kinase

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

The smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). It functions by mimicking the substrate and competitively inhibiting the binding of the natural substrate to the enzyme, thereby reducing kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, which subsequently impedes muscle contraction.

Myosin-5-IN-2 (Compound G19) is an inhibitor of Myosin-5 that exhibits antifungal activity against Fusarium graminearum (Fg), Botrytis cinerea, and Rhizoctonia solani, with an EC50 of 0.326 μg/mL for Fg. It is effective in protecting and treating wheat leaves, severely disrupting the surface integrity of hyphal cells and inducing cytoplasmic leakage. Myosin-5-IN-2 is useful for studying fungal infections, such as Fusarium head blight (FHB).

Myosin-IN-2 (Example 16) is an inhibitor of Myosin ATPase, exhibiting an IC50 value of 1.06 μM. It is applicable in research related to cardiac diseases, including hypertrophic cardiomyopathy (HCM).

Myosin-IN-5 (Example 3) is a myosin inhibitor with an IC50 of 1.84 μM against bovine cardiac myosin. It demonstrates strong selectivity between cardiac and skeletal muscle myosins, exhibiting IC50 values of 43.4 μM for bovine cardiac myofibrils and 1.5 μM for rabbit skeletal muscle myofibrils. This compound is useful in researching hypertrophic cardiomyopathy (HCM).