Myosin Inhibitor

E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activities of calmodulin-dependent myosin light chain kinase (MLCK) and phosphodiesterase (PDE). E6 Berbamine exhibits anti-leukemic activity. E6 Berbamine can be used in research related to cardiovascular abnormalities and chronic myeloid leukemia.

JB062 is a nonmuscle myosin inhibitor with IC₅₀ values of 1.6, 5.4, and >100 μM for Skeletal muscle myosin, Cardiac muscle myosin, and Smooth muscle myosin II, respectively. JB062 has cytotoxic to human cancer cells but not normal cells. JB062 can be used in research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). The smMLCK peptide mimics the substrate and competitively inhibits the binding of the actual substrate to the enzyme, thereby inhibiting the kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, thus inhibiting muscle contraction.

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.

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-3 (Compound 4-1) is a pyrimidine ketone derivative. Myosin-IN-3 exhibits significant anti ferroptotic activity (IC₅₀ = 3.11 μM) while possessing myosin (IC₅₀ = 3.09 μM) inhibitory activity and antioxidant activity (DPPH EC₅₀ = 23.17 μM; MDA EC₅₀ = 55.34 μM). Myosin-IN-3 can be used for research on heart conditions such as hypertrophic cardiomyopathy.

(S)-3'-Aminoblebbistatin is the derivative of Blebbistatin (HY-13813). (S)-3'-Aminoblebbistatin exhibits inhibitory activity against myosin II with an IC₅₀ of 14.1 µM.

1α-Hydroxyvitamin D5 (CARD-024) is a vitamin D analog with extremely low hypercalcemic effects. 1α-Hydroxyvitamin D5 effectively attenuates the pro-fibrotic response of colonic myofibroblasts to TGFβ and high-stiffness substrates by inhibiting the expression of αSMA, the phosphorylation of FAK, and the gene expression of MLCK and ET-1, while activating the anti-inflammatory pathway of IL-1β/COX-2. 1α-Hydroxyvitamin D5 can be used in research related to intestinal fibrosis associated with Crohn's disease.

JB002 is a myosin II inhibitor, with an IC₅₀ of ≤10 μM. JB002 can be used for the research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

MT-134 is a SkMII-specific inhibitor and has excellent exposure in muscles.

HA-100 hydrochloride 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 hydrochloride also used as a ROCK inhibitor.

CK-571 is a potent and selective inhibitor of smooth muscle myosin-2 (SMM), with an IC₅₀ value of 86 nM. CK-571 exhibits IC₅₀ values for cardiac muscle myosin (CMM), skeletal muscle myosin (SKM), and non-muscle myosin-2A (NMM-2A) of 2.3, 42, and 0.58 μM, respectively. CK-571 can be used for research on asthma, chronic obstructive pulmonary disease, and other smooth muscle-related diseases.

Myosin I-IN-1 is an Antifungal agent and Myosin I inhibitor with a K_d of 0.14 μM for FgMyoI. Myosin I-IN-1 inhibits mycelial growth, sporulation, spore germination, and Deoxynivalenol (HY-N6684) biosynthesis. Myosin I-IN-1 disrupts cell wall and cell membrane integrity and induces hyphal morphological changes. Myosin I-IN-1 exhibits broad-spectrum antifungal activity against plant pathogenic fungi. Myosin I-IN-1 shows protective efficacy against Fusarium head blight in wheat and maize. Myosin I-IN-1 can be used for research on Fusarium head blight.

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.

(-)-Blebbistatin (GMP) is (-)-Blebbistatin (HY-13441) produced by using GMP guidelines. (-)-Blebbistatin (GMP) is a selective inhibitor of the ATPase activity of non-muscle myosin II.

Diazobenzenesulfonic acid (4-Sulfobenzenediazonium) is an inhibitor of aliostericeffect for myosin ATPase 13.

HA-100 dihydrochloride 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 dihydrochloride also used as a ROCK inhibitor.

Myokinasib-II is a MLCK1 inhibitor with an IC₅₀ of 4.4 μM. Myokinasib-II induces cell cortex softening, impairs cell migration capacity, induces multinucleation, reduces cell stiffness, alters membrane tether dynamics, decreases actomyosin tension and changes nuclear morphology. Myokinasib-II is a MLCK1 chemical biology probe with a unique structure that does not depolymerize tubulin and maintains cell viability even under high-concentration treatment in fibroblasts.

MS-347a is an inhibitor of myosin light chain kinase (MLCK) and protein kinase C (PKC), with IC₅₀ values of 9.2 μM, 31 μM and 16 μM against calmodulin-dependent MLCK, calmodulin-independent MLCK and PKC, respectively. MS-347a binds to the catalytic domain of MLCK and blocks both calmodulin-dependent and calmodulin-independent MLCK activity. MS-347a inhibits the growth of drug-sensitive fission yeast and multiple ascomycete phytopathogenic fungi. MS-347a exhibits fungicidal activity against a variety of phytopathogenic fungi and protective activity against Magnaporthe oryzae in rice seedlings. MS-347a shows antibacterial activity against specific Gram-positive bacteria and Proteus vulgaris. MS-347a can be used in studies related to rice blast, bacterial infections and phytopathogenic fungal diseases.

Adhibin is an allosteric inhibitor for RhoGAP class IX myosin, that inhibits Myo9 ATPase in mammalian and invertebrate with IC₅₀ of 2.5 µM and 2.6 µM. Adhibin binds to the ATPase of myosin, interfers with its motor function, blocks the RhoGTPase related signaling pathway, and affects the cell migration, adhesion and cell division. Adhibin can be used in research about cancer metastasis.