CaMK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/CaMK.html CaMKCalmodulin-dependent protein kinases; Calmodulin-dependent kinasesThe Ca2+/calmodulin-dependent kinase (CaMK) family has been recognized as a key mediator in living organisms and variousbiological processes.CaMK II is a multifunctional cytoplasmic

2、 calcium and calmodulin-dependent protein kinase that phosphorylates and alters thefunction of a variety of substrates. The CaMK II pathway has been found to regulate the RANKL-induced osteoclast formation viathe cAMP-response element binding protein (CREB) pathway.Among many signaling pathways of p

3、roliferation, intracellular calciumol/L has been extensively demonstrated to be very important.In cytoplasm, calciumol/L binds to calmodulin, and then activates the CaMKs which are a family of structurally relatedserine/threonine protein kinases including CaMKI-IV. CaMKII, a multi functional protein

4、 kinase, is ubiquitously involved in manyphysiological processes including control of cell cycle, apoptosis, gene expression, and neurotransmission.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/CaMK.html CaMK HYPERLINK https:/www.MedChemE/Targets/CaMK.html HYPERLINK https:/www.MedChemE/Target

5、s/CaMK.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/CaMK.html HYPERLINK https:/www.MedChemE/Targets/CaMK.html & HYPERLINK https:/www.MedChemE/Targets/CaMK.html HYPERLINK https:/www.MedChemE/Targets/CaMK.html Antagonists HYPERLINK https:/www.MedChemE/a-3-hydrochloride.html A-3 HYPERLINK http

6、s:/www.MedChemE/a-3-hydrochloride.html HYPERLINK https:/www.MedChemE/a-3-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/a-3-hydrochloride.html HYPERLINK https:/www.MedChemE/A-484954.html A-484954Cat. No.: HY-125957 Cat. No.: HY-110096A-3 hydrochloride is a potent, cell-permeable,reve

7、rsible, ATP-competitive non-selectiveantagonist of various kinases. It against PKA(Ki=4.3 M), casein kinase II (Ki=5.1 M) andmyosin light chain kinase (MLCK) (K=7.4 M).iA-484954 is a highly selective eukaryoticelongationfactor-2 (eEF2) inhibitor, with an ICof 280 nM.50Purity: 99.67%Clinical Data: No

8、 Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/acremonidin-a.html Acremonidin HYPERLINK https:/www.MedChemE/acremonidin-a.html HYPERLINK https:/www.MedChemE/acrem

9、onidin-a.html A HYPERLINK https:/www.MedChemE/acremonidin-a.html HYPERLINK https:/www.MedChemE/acremoxanthone-c.html Acremoxanthone HYPERLINK https:/www.MedChemE/acremoxanthone-c.html HYPERLINK https:/www.MedChemE/acremoxanthone-c.html CCat. No.: HY-N10198 Cat. No.: HY-N10199Acremonidin A is a poten

10、t calmodulin (CaM)inhibitor found in Purpureocilliumlilacinum. Acremonidin A binds to the humancalmodulin (hCaM) biosensor hCaM M124C-mBBr, withK of 19.40 nM.dAcremoxanthone C is a potent calmodulin(CaM) inhibitor found in Purpureocilliumlilacinum. Acremoxanthone C binds to the humancalmodulin (hCaM

11、) biosensor hCaM M124C-mBBr, withK of 18.25 nM.dPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Autocamtide_2.html Autocamtide HYPERLINK https:/www.MedChemE/Autocamtide_2.html HYPERLINK h

12、ttps:/www.MedChemE/Autocamtide_2.html 2(Autocamtide II) Cat. No.: HY-P0225 HYPERLINK https:/www.MedChemE/Autocamtide_2,_amide.html Autocamtide HYPERLINK https:/www.MedChemE/Autocamtide_2,_amide.html HYPERLINK https:/www.MedChemE/Autocamtide_2,_amide.html 2, HYPERLINK https:/www.MedChemE/Autocamtide_

13、2,_amide.html HYPERLINK https:/www.MedChemE/Autocamtide_2,_amide.html amideCat. No.: HY-P1528Autocamtide 2 is a highly selective peptidesubstrate of calcium/calmodulin-dependent proteinkinase II (CaMKII). It can be used in theCaMKII activity assay.Autocamtide 2, amide is a substrate (100 M finalconc

14、entration) for CaMK family assays.Purity: 98.21%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.47%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide.html Autocamtide-2-related HYPERLINK https:/www.Med

15、ChemE/autocamtide-2-related-inhibitory-peptide.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide.html inhibitory HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide.html peptide H

16、YPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide.html HYPERLINK https:/www.MedChemE/Autocamtide-2-related_inhibitory_peptide_TFA.html Autocamtide-2-related HYPERLINK https:/www.MedChemE/Autocamtide-2-related_inhibitory_peptide_TFA.html HYPERLINK https:/www.MedChemE/Autocamtide-2

17、-related_inhibitory_peptide_TFA.html inhibitory HYPERLINK https:/www.MedChemE/Autocamtide-2-related_inhibitory_peptide_TFA.html HYPERLINK https:/www.MedChemE/Autocamtide-2-related_inhibitory_peptide_TFA.html peptide HYPERLINK https:/www.MedChemE/Autocamtide-2-related_inhibitory_peptide_TFA.html HYPE

18、RLINK https:/www.MedChemE/Autocamtide-2-related_inhibitory_peptide_TFA.html TFACat. No.: HY-P0214 Cat. No.: HY-P0214AAutocamtide-2-related inhibitory peptide is ahighly specific and potent inhibitor of CaMKIIwith an IC of 40 nM.50Autocamtide-2-related inhibitory peptide (TFA) isa highly specific and

19、 potent inhibitor ofCaMKII with an IC of 40 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.85%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html Autocamtide-2-related HYPER

20、LINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html inhibitory HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html HYPERLINK https:/www.Med

21、ChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html peptide, HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated.html myristoylated HYPERLINK https:/www.MedChemE/a

22、utocamtide-2-related-inhibitory-peptide-myristoylated.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html Autocamtide-2-related HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html HYPERLINK https:/www.MedChemE/a

23、utocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html inhibitory HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html peptide, HYPERLINK https:/www.MedChemE

24、/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html myristoylated HYPERLINK https:/www.MedChemE/autocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html HYPERLINK https:/www.MedChemE/aut

25、ocamtide-2-related-inhibitory-peptide-myristoylated-tfa.html TFACat. No.: HY-P0215 Cat. No.: HY-P0215AAutocamtide-2-related inhibitory peptide,myristoylated is the myristoylatedAutocamtide-2-related inhibitory peptide.Autocamtide-2-related inhibitory peptide is ahighly specific and potent inhibitor

26、of CaMKIIwith an IC of 40 nM.50Autocamtide-2-related inhibitory peptide,myristoylated TFA is the myristoylatedAutocamtide-2-related inhibitory peptide.Autocamtide-2-related inhibitory peptide is ahighly specific and potent inhibitor of CaMKIIwith an IC of 40 nM.50Purity: 98%Clinical Data: No Develop

27、ment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Calmidazolium_chloride.html Calmidazolium HYPERLINK https:/www.MedChemE/Calmidazolium_chloride.html HYPERLINK https:/

28、www.MedChemE/Calmidazolium_chloride.html chloride(R 24571) Cat. No.: HY-103319 HYPERLINK https:/www.MedChemE/calmodulin-antagonist-1.html Calmodulin HYPERLINK https:/www.MedChemE/calmodulin-antagonist-1.html HYPERLINK https:/www.MedChemE/calmodulin-antagonist-1.html antagonist-1Cat. No.: HY-115745Ca

29、lmidazolium chloride (R 24571) is acalmodulin (CaMK) antagonist, antagonizingCaM-dependent phosphodiesterase andcalmodulin-induced activation of erythrocyteCa2+-transporting ATPase with IC s of 0.15 and500.35 M, respectively.Calmodulin antagonist-1 (W-7) is a calmodulin(CaM) antagonist. Calmodulin a

30、ntagonist-1inhibits calmodulin-activatedCa2+-phosphodiesterase (PDE) (IC =28 M).50Purity: 98.93%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinas

31、e_II_290-309.html Calmodulin-Dependent HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html Protein HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html HYPERLI

32、NK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html Kinase HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html II HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_

33、Protein_Kinase_II_290-309.html HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html (290-309) HYPERLINK https:/www.MedChemE/Calmodulin-Dependent_Protein_Kinase_II_290-309.html HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html Calmo

34、dulin-Dependent HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html Protein HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html HYPERL

35、INK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html Kinase HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html II(290-309) HYPERLINK https:/

36、www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html HYPERLINK https:/www.MedChemE/calmodulin-dependent-protein-kinase-ii-290-309-acetate.html acetateCat. No.: HY-P1479 Cat. No.: HY-P1479ACalmodulin-Dependent Protein Kinase II (290-309)is a potent CaMK antagonist with an IC of 52

37、50nM for inhibition of Ca2+/calmodulin-dependentprotein kinase II.Calmodulin-Dependent Protein Kinase II (290-309)acetate is a potent CaMK antagonist with anIC of 52 nM for inhibition of50Ca2+/calmodulin-dependent protein kinase II.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPur

38、ity: 98.97%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CaMKII-IN-1.html CaMKII-IN-1Cat. No.: HY-18271 HYPERLINK https:/www.MedChemE/ddd107498.html DDD107498(DDD-498; M5717) Cat. No.: HY-117684CaMKII-IN-1 is a potent and highly selectiveCaMKII inhibitor with I

39、C50 of 63 nM; significantlyhigh selectivity against CaMKIV, MLCK, p38a, Akt1,and PKC. IC50 value: 63 nM Target: CaMKII.DDD107498 (DDD-498) is a potent and orally activeantimalarial agent, inhibits multiplelife-cycle stages of the parasite, with an EC50of 1 nM against P. falciparum 3D7.Purity: 99.74%

40、Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.33%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/ddd107498-succinate.html DDD107498 HYPERLINK https:/www.MedChemE/ddd107498-succinate.html HYPERLINK http

41、s:/www.MedChemE/ddd107498-succinate.html succinate HYPERLINK https:/www.MedChemE/ddd107498-succinate.html HYPERLINK https:/www.MedChemE/glycyl-h-1152-hydrochloride.html Glycyl HYPERLINK https:/www.MedChemE/glycyl-h-1152-hydrochloride.html HYPERLINK https:/www.MedChemE/glycyl-h-1152-hydrochloride.htm

42、l H-1152 HYPERLINK https:/www.MedChemE/glycyl-h-1152-hydrochloride.html HYPERLINK https:/www.MedChemE/glycyl-h-1152-hydrochloride.html hydrochloride(DDD-498 succinate) Cat. No.: HY-117684ACat. No.: HY-15720BDDD107498 succinate (DDD-498 succinate) is apotent and orally active antimalarial agent,inhib

43、its multiple life-cycle stages of theparasite, with an EC of 1 nM against50 P.falciparum 3D7.Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride. Glycyl H-1152 hydrochlorideinhibits ROCKII, Aurora A, CAMKII and PKG,with IC s of 0.0118, 2.35,

44、 2.57 and 3.26 M50respectively.Purity: 99.99%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 mg HYPERLINK https:/www.MedChemE/k-252a.html K-252a HYPERLINK https:/www.MedChemE/k-252a.html HYPERLINK

45、 https:/www.MedChemE/KN-62.html KN-62(SF2370; Antibiotic K 252a; Antibiotic SF 2370) Cat. No.: HY-N6732Cat. No.: HY-13290K-252a, a staurosporine analog, inhibits proteinkinase, with IC values of 470 nM, 140 nM, 270 nM,50and 1.7 nM for PKC, PKA,Ca2+/calmodulin-dependent kinase type II, andphosphoryla

46、se kinase, respectively.KN-62 is a selective and reversible inhibitor ofcalmodulin-dependent protein kinase II(CaMK-II) with a K of 0.9 M for rat brainiCaMK-II. KN-62 directly binds to the calmodulinbinding site of CaMK-II.Purity: 99.45%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5

47、 mgPurity: 99.45%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/KN-93.html KN-93 HYPERLINK https:/www.MedChemE/KN-93.html HYPERLINK https:/www.MedChemE/KN-93-hydrochloride.html KN-93 HYPERLINK https:/www.MedChemE/KN-93-hydrochlo

48、ride.html HYPERLINK https:/www.MedChemE/KN-93-hydrochloride.html hydrochlorideCat. No.: HY-15465 Cat. No.: HY-15465AKN-93 is a cell-permeable, reversible andcompetitive inhibitor calmodulin-dependent kinasetype II (CaMKII) with a K of 370 nM.iKN-93 hydrochloride is a cell-permeable,reversible and co

49、mpetitive inhibitorcalmodulin-dependent kinase type II (CaMKII)with a K of 370 nM.iPurity: 99.19%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK http

50、s:/www.MedChemE/KN-93-phosphate.html KN-93 HYPERLINK https:/www.MedChemE/KN-93-phosphate.html HYPERLINK https:/www.MedChemE/KN-93-phosphate.html phosphate HYPERLINK https:/www.MedChemE/KN-93-phosphate.html HYPERLINK https:/www.MedChemE/lavendustin-c.html Lavendustin HYPERLINK https:/www.MedChemE/lav

51、endustin-c.html HYPERLINK https:/www.MedChemE/lavendustin-c.html CCat. No.: HY-15465B Cat. No.: HY-W013857KN-93 phosphate is a novel membrane-permeantsynthetic inhibitor of purified neuronalCaMK-II, with K of 370 nM.iLavendustin C is a potent Ca2+calmodulin-dependent kinase II (CaMK II) inhibitorwit

52、h an IC of 0.2 M. Lavendustin C inhibits50EGFR-associated tyrosine kinase (IC =0.012 M) and50pp60c-src(+) kinase (IC =0.5 M) .50Purity: 99.69%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK ht

53、tps:/www.MedChemE/Metofenazate.html Metofenazate(Methophenazine) Cat. No.: HY-100263 HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html MLCK HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html inhibitor HYPERLINK https:/

54、www.MedChemE/MLCK_inhibitor_peptide_18.html HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html peptide HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html HYPERLINK https:/www.MedChemE/MLCK_inhibitor_peptide_18.html 18Cat. No.: HY-P1029Metofenazate is a selective calmodulininhibit

55、or.MLCK inhibitor peptide 18 is a myosin light chainkinase (MLCK) inhibitor with an IC of 50 nM,50and inhibits CaM kinase II only at 4000-foldhigher concentrations.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.66%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 1

56、0 mg, 25 mg HYPERLINK https:/www.MedChemE/NH125.html NH125 HYPERLINK https:/www.MedChemE/NH125.html HYPERLINK https:/www.MedChemE/psoralenoside.html PsoralenosideCat. No.: HY-100576 Cat. No.: HY-N7503NH125 is a potent and selective inhibitor ofeukaryotic elongation factor 2 kinase(eEF-2K/CaMKIII), a

57、lso can induce eEF2phosphorylation, with an IC of 60 nM for eEF-2K.50Psoralenoside is a benzofuran glycoside fromPsoralea corylifolia. Psoralenoside exhibits highbinding affinities against histaminergic H ,1calmodulin, and voltage-gated L-type calciumchannels (E-value-6.5 Kcal/mol).Purity: 98.0%Clin

58、ical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Rimacalib.html Rimacalib HYPERLINK https:/www.MedChemE/Rimacalib.html HYPERLINK https:/www.MedChemE/sordarin-sodium.ht

59、ml Sordarin HYPERLINK https:/www.MedChemE/sordarin-sodium.html HYPERLINK https:/www.MedChemE/sordarin-sodium.html sodium(SMP 114) Cat. No.: HY-100779Cat. No.: HY-126396Rimacalib (SMP 114) is aCa2+/calmodulin-dependent protein kinase II(CaMKII) inhibitor, with IC s of 1 M for50CaMKII to 30 M for CaMK

60、II.Sordarin is a potent diphthamide-dependent eEF2inhibitor with antifungal properties. Sordarintargets eEF2 so as to inhibit protein translationby blocking eEF2-mediated translocation of tRNAs.Purity: 99.65%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No De