Myosin-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Myosin.html MyosinMyosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force. This enablesmyosins to propel the sliding of actin filaments, to produce tension on actin filaments and to walk along these filamen

2、ts. As aresult, myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components. The different myosins are grouped into classes on the basis of their motor domains. There are 35 knownclasses of myosin, and humans have 40 myosi

3、n genes that fall into 13 classes (I, II, III, V, VI, VII, IX, X, XV, XVI, XVIII, XIX and XXXV).Myosins are actin-dependent motors that participate in a diverse range of crucial activities, including muscle contraction,intracellular trafficking, cell division, motility, actin cytoskeletal organisati

4、on and cell signaling. Myosin malfunction has beenimplicated in a variety of disorders including deafness, hypertrophic cardiomyopathy, Usher syndrome, Griscelli syndrome andcancer.Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cy

5、toskeletoncontraction and tight junction regulation. In most cells, MLCK is a transducer for signalling MLC phosphorylation in response to Ca2+ binding to MLCK-associated calmodulin. MLCK-mediated MLC phosphorylation and actomyosin contractility is important inmuscle contraction, cell migration, and

6、 endo/exocytic processes, and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Myosin.html Myosin HYPERLINK https:/www.MedChemE/Targets/Myosin.html HYPERLINK https:/www.MedChemE/Targets/Myosin.htm

7、l Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Myosin.html HYPERLINK https:/www.MedChemE/Targets/Myosin.html Activators HYPERLINK https:/www.MedChemE/Targets/Myosin.html HYPERLINK https:/www.MedChemE/Targets/Myosin.html & HYPERLINK https:/www.MedChemE/Targets/Myosin.html HYPERLINK https:/www.Me

8、dChemE/Targets/Myosin.html Modulators HYPERLINK https:/www.MedChemE/plus-blebbistatin.html (+)-BlebbistatinCat. No.: HY-107657 HYPERLINK https:/www.MedChemE/_-_-Blebbistatin.html (-)-Blebbistatin(S)-(-)-Blebbistatin) Cat. No.: HY-13441(+)-Blebbistatin is the inactive enantiomer of()-Blebbistatin. ()

9、-Blebbistatin is a selectiveinhibitor of myosin II ATPase.(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.42%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg HYPERLINK ht

10、tps:/www.MedChemE/aficamten.html Aficamten(CK-274; CK-3773274) Cat. No.: HY-139465 HYPERLINK https:/www.MedChemE/ATM-3507.html ATM-3507Cat. No.: HY-100948Aficamten (CK-274) is a potent cardiac myosininhibitor with an IC of 1.4 M. Aficamten can be50used for the research of hypertrophiccardiomyopathy

11、(HCM).ATM-3507 is a potent tropomyosin inhibitor withIC s from 3.83-6.84 M in human melanoma cell50lines.Purity: 99.86%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/atm-3507

12、-trihydrochloride.html ATM-3507 HYPERLINK https:/www.MedChemE/atm-3507-trihydrochloride.html HYPERLINK https:/www.MedChemE/atm-3507-trihydrochloride.html trihydrochloride HYPERLINK https:/www.MedChemE/atm-3507-trihydrochloride.html HYPERLINK https:/www.MedChemE/blebbistatin.html BlebbistatinCat. No.

13、: HY-100948B Cat. No.: HY-13813ATM-3507 trihydrochloride is a potenttropomyosin inhibitor with IC s from 3.83-6.8450M in human melanoma cell lines.Blebbistatin is a selective non-muscle myosinII (NMII) inhibitor, promotes directionalmigration of corneal endothelial cells (CECs) andaccelerates wound

14、healing, and better preservescell junctional integrity and barrier function.Purity: 98.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.64%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/BT

15、S.html BTS HYPERLINK https:/www.MedChemE/BTS.html HYPERLINK https:/www.MedChemE/danicamtiv.html Danicamtiv(N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine) Cat. No.: HY-16690 (MYK-491) Cat. No.: HY-109128BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myos

16、inII subfragment 1 (S1) ATPase activity, with anIC s of 5 M for actin- and Ca -stimulated2+50myosin S1 ATPase. BTS specifically inhibits thecontraction of fast skeletal muscle fibers.Danicamtiv (MYK-491), an inotropic agent, is aselective allosteric activator of cardiacmyosin. Danicamtiv increases c

17、ardiac systolicfunction and preserves mechanical efficiency.Purity: 99.51%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 500 mgPurity: 99.49%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/HA-100.html HA-100 HYPERLINK https:/www.MedChe

18、mE/HA-100.html HYPERLINK https:/www.MedChemE/ha-100-hydrochloride.html HA-100 HYPERLINK https:/www.MedChemE/ha-100-hydrochloride.html HYPERLINK https:/www.MedChemE/ha-100-hydrochloride.html hydrochlorideCat. No.: HY-100984 Cat. No.: HY-100984AHA-100 is a potent protein kinase inhibitor, withIC s of

19、4 M, 8 M, 12 M and 240 M for50cGMP-dependent protein kinase (PKG),cAMP-dependent protein kinase (PKA), proteinkinase C (PKC) and MLC-kinase, respectively.HA-100 also used as a ROCK inhibitor.HA-100 hydrochloride is a potent protein kinaseinhibitor, with IC s of 4 M, 8 M, 12 M and 24050M for cGMP-dep

20、endent protein kinase (PKG),cAMP-dependent protein kinase (PKA), proteinkinase C (PKC) and MLC-kinase, respectively.Purity: 99.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6

21、898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Mavacamten.html Mavacamten(MYK461; SAR439152) Cat. No.: HY-109037 HYPERLINK https:/www.MedChemE/ML-7-hydrochloride.html ML-7 HYPERLINK https:/www.MedChemE/ML-7-hydrochloride.html HYPERLINK https:/www.MedChemE/ML-7-hydrochloride

22、.html hydrochlorideCat. No.: HY-15417Mavacamten (MYK461) is an orally active modulatorof cardiac myosin, with IC s of 490, 711 nM for50bovine cardiac and human cardiac, respectively.ML-7 hydrochloride is a naphthalene sulphonamidederivative, potently inhibits MLCK (IC =30050nM). ML-7 hydrochloride a

23、lso inhibits YAP/TAZ.Purity: 99.90%Clinical Data: Phase 3Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/ml-9.html ML-9 HYPERLINK https:/www.MedChemE/ml-9.html HYPERLINK https:/www.MedCh

24、emE/ml-9-free-base.html ML-9 HYPERLINK https:/www.MedChemE/ml-9-free-base.html HYPERLINK https:/www.MedChemE/ml-9-free-base.html Free HYPERLINK https:/www.MedChemE/ml-9-free-base.html HYPERLINK https:/www.MedChemE/ml-9-free-base.html BaseCat. No.: HY-100932 Cat. No.: HY-100932AML-9 is a selective an

25、d potent inhibitor of Aktkinase, inhibits myosin light-chain kinase (MLCK)and stromal interaction molecule 1 (STIM1)activity. ML-9 inhibits inhibits MLCK, PKA and PKCactivity with K values of 4, 32 and 54 M,irespectively.ML-9 (Free Base) is a selective and potentinhibitor of Akt kinase, inhibits myo

26、sinlight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity.Purity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 25 mg, 50 mg, 100 mg, 250 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.

27、html MLCK HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html inhibitor HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html peptide HYPERLINK https:/www.MedChem

28、E/MLCK_inhibitor_peptide_18.html HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html 18Cat. No.: HY-P1029 HYPERLINK https:/www.MedChemE/MS-444.html MS-444(BE-34776) Cat. No.: HY-100685MLCK inhibitor peptide 18 is a myosin light chainkinase (MLCK) inhibitor with an IC of 50 nM,50and inhibits

29、 CaM kinase II only at 4000-foldhigher concentrations.MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase (MLCK) with anIC value of 10 M.50Purity: 99.66%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mgPurity: 99.42%Clinical Data: No Development Reporte

30、dSize: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/mt-134.html MT-134 HYPERLINK https:/www.MedChemE/mt-134.html HYPERLINK https:/www.MedChemE/Omecamtiv-mecarbil.html Omecamtiv HYPERLINK https:/www.MedChemE/Omecamtiv-mecarbil.html HYPERLINK https:/www.MedChemE/Omecamtiv-mecarbil.html mecarbilCat.

31、No.: HY-141810(CK-1827452) Cat. No.: HY-14233MT-134 is a SkMII-specific inhibitor and hasexcellent exposure in muscles.Omecamtiv mecarbil (CK-1827452) is a selectivecardiac myosin activator.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.89%Clinical Data: Phase 3Size: 10

32、mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/omecamtiv-mecarbil-d8.html Omecamtiv HYPERLINK https:/www.MedChemE/omecamtiv-mecarbil-d8.html HYPERLINK https:/www.MedChemE/omecamtiv-mecarbil-d8.html mecarbil-d8 HYPERLINK https:/www.MedChemE/omecamtiv-mecarbil-d8.html HYPERLI

33、NK https:/www.MedChemE/para-nitroblebbistatin.html para-Nitroblebbistatin(CK-1827452-d8) Cat. No.: HY-14233SCat. No.: HY-120870Omecamtiv mecarbil-d8 (CK-1827452-d8) is thedeuterium labeled Omecamtiv mecarbil. Omecamtivmecarbil (CK-1827452) is a selective cardiacmyosin activator.para-Nitroblebbistatin is a non-cytotoxic,photostable, fluorescent and specific Myosin IIinhibitor, usd in the study of the specific roleof myosin II in physiological, developmental, andcell biological studies.Purity: 98%Clinical Data: No Development