Cathepsin-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Cathepsin.html CathepsinCathepsins are protease enzymes, categorized into multiple families. Cathepsins can be serine protease, cysteine protease, oraspartyl protease. There are about 15 classes of cathepsins in humans (Cathepsin A, B, C, D, E, F, G, H, K, L, O

2、, S, V, W, and Z).Cathepsins are active in the low pH milieu of lysosomes and are versatile in their functions. Like other enzymes, they are vital for thenormal physiological functions such as digestion, blood coagulation, bone resorption, ion channel activity, innate immunity,complement activation,

3、 apoptosis, vesicular trafficking, autophagy, angiogenesis, proliferation, and metastasis, among scores ofothers.Numerous pathologies have been attributed to the dysregulated cathepsins, some of which include arthritis, periodontitis,pancreatitis, macular degeneration, muscular dystrophy, atheroscle

4、rosis, obesity, stroke, Alzheimers disease, schizophrenia,tuberculosis, and Ebola.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Cathepsin.html Cathepsin HYPERLINK https:/www.MedChemE/Targets/Cathepsin.html HYPERLINK https:/www.MedChemE/Targets/Cathepsin.html Inhibitors HYPERLINK https:/www.Me

5、dChemE/2-cyanopyrimidine.html 2-Cyanopyrimidine HYPERLINK https:/www.MedChemE/2-cyanopyrimidine.html HYPERLINK https:/www.MedChemE/3-epiursolic-acid.html 3-Epiursolic HYPERLINK https:/www.MedChemE/3-epiursolic-acid.html HYPERLINK https:/www.MedChemE/3-epiursolic-acid.html AcidCat. No.: HY-Y0241 Cat.

6、 No.: HY-N42892-Cyanopyrimidine is a potent and non-selectivecysteine protease cathepsin K inhibitor with anIC of 170 nM. 2-Cyanopyrimidine is used for50osteoporos.3-Epiursolic Acid is a triterpenoid isolated fromMyrtaceae, acts as a competitive inhibitor ofcathepsin L (ICIC , 6.5 M; , 19.5 M), with

7、 no50 Kiobvious effect on cathepsin B.Purity: 99.92%Clinical Data: No Development ReportedSize: 100 mgPurity: 99.49%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/abp-25.html ABP HYPERLINK https:/www.MedChemE/abp-25.html HYPERLINK https:/www.MedChemE/abp

8、-25.html 25Cat. No.: HY-139685 HYPERLINK https:/www.MedChemE/allm.html ALLM(Calpain inhibitor II) Cat. No.: HY-118355ABP 25 is an activity-based probe for cathepsin Kimaging with excellent potency and selectivity.ALLM (Calpain inhibitor II) is a potent inhibitorof calpain and cathepsin proteases. AL

9、LM inhibitsneuronal cell death and improves chronicneurological function after spinal cord injury(SCI).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Aloxistatin.html Aloxistatin(E64d; E

10、64c ethyl ester) Cat. No.: HY-100229 HYPERLINK https:/www.MedChemE/asperphenamate.html AsperphenamateCat. No.: HY-129578Aloxistatin (E64d) is a cell-permeable andirreversible broad-spectrum cysteine proteaseinhibitor. Aloxistatin (E64d) exhibitsentry-blocking effect for MERS-CoV.Asperphenamate, a fu

11、ngal metabolite of Aspergillusflatiipes with anti-cancer effect, exhibits IC50values of 92.3 M, 96.5 M and 97.9 M in T47D,MDA-MB-231 and HL-60 cells, respectively.Purity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Dev

12、elopment ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/atg4b-in-2.html Atg4B-IN-2 HYPERLINK https:/www.MedChemE/atg4b-in-2.html HYPERLINK https:/www.MedChemE/aurantiamide-acetate.html Aurantiamide HYPERLINK https:/www.MedChemE/aurantiamide-acetate.html HYPERLINK https:/www.MedChemE/auranti

13、amide-acetate.html acetateCat. No.: HY-144636(Asperglaucide) Cat. No.: HY-N2905Atg4B-IN-2 is a potent competitive Atg4Binhibitor with K value of 3.1 M, also possessesideclining PLA2 inhibitory potency, IC50s of 11M and 3.5 M for Atg4B and PLA , respectively.2Aurantiamide acetate (TMC-58A) is a selec

14、tive andorally active cathepsin inhibitor isolatedfrom Portulaca oleracea L. Aurantiamideacetate has anti-inflammatory activities and canbe used for the study ofinflammatory diseases.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.24%Clinical Data: No Development Reported

15、Size: 5 mg HYPERLINK https:/www.MedChemE/Balicatib.html Balicatib HYPERLINK https:/www.MedChemE/Balicatib.html HYPERLINK https:/www.MedChemE/CA-074.html CA-074(AAE581) Cat. No.: HY-15100Cat. No.: HY-103350Balicatib(AAE-581) is a potent and selectiveinhibitor of cathepsin K; 10-100 fold more potentin

16、 cell-based enzyme occupancy assays than againstcathepsin B, L, and S.CA-074 is a potent inhibitor of cathepsin B with aK of 2 to 5 nM.iPurity: 99.07%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10

17、 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/CA-074-methyl-ester.html CA-074 HYPERLINK https:/www.MedChemE/CA-074-methyl-ester.html HYPERLINK https:/www.MedChemE/CA-074-methyl-ester.html methyl HYPERLINK https:/www.MedChemE/CA-074-methyl-ester.html HYPE

18、RLINK https:/www.MedChemE/CA-074-methyl-ester.html ester(CA-074Me) Cat. No.: HY-100350 HYPERLINK https:/www.MedChemE/Calpeptin.html CalpeptinCat. No.: HY-100223CA-074 methyl ester is a specific inhibitor ofCathepsin B, which has potent bioactivities suchas neuroprotective, anti-cancer, andanti-infla

19、matory effects.Calpeptin is a potent, cell penetrating calpaininhibitor, with an ID of 40 nM for Calpain I in50human platelets. Calpeptin is also an inhibitor ofcathepsin K.Purity: 99.15%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mgPurity: 98.0%Clinical Data: No De

20、velopment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html Cathepsin HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html D HYPERLINK http

21、s:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html and HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html E HYPERLINK https:/www.MedChemE/cathep

22、sin-d-and-e-fret-substrate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html FRET HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate.html Substrate HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-f

23、ret-substrate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html Cathepsin HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html D HYPERLINK https:/www.MedChemE/cathepsin-d

24、-and-e-fret-substrate-acetate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html and HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html E HYPERLINK https:/www.MedChemE/c

25、athepsin-d-and-e-fret-substrate-acetate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html FRET HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html Substrate HYPERLINK ht

26、tps:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html HYPERLINK https:/www.MedChemE/cathepsin-d-and-e-fret-substrate-acetate.html acetateCat. No.: HY-P2498 Cat. No.: HY-P2498ACathepsin D and E FRET Substrate is a fluorogenicsubstrate for cathepsins D and E and not for B, Hor L. The cleavag

27、e occurs at the Phe-Phe amidebond resul. Cathepsin D and E FRET Substrate is avaluable tool for routine assays and formechanistic studies on cathepsins E and D.Cathepsin D and E FRET Substrate acetate is afluorogenic substrate for cathepsins D and E andnot for B, H or L. The cleavage occurs at thePh

28、e-Phe amide bond resul. Cathepsin D and E FRETSubstrate is a valuable tool for routine assaysand for mechanistic studies on cathepsins E and D.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.06%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https

29、:/www.MedChemE/cathepsin-g-inhibitor-i.html Cathepsin HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html G HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html Inhibito

30、r HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html I HYPERLINK https:/www.MedChemE/cathepsin-g-inhibitor-i.html HYPERLINK https:/www.MedChemE/cathepsin-inhibitor-1.html Cathepsin HYPERLINK https:/www.MedChemE/cathepsin-inhibitor-1.

31、html HYPERLINK https:/www.MedChemE/cathepsin-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/cathepsin-inhibitor-1.html HYPERLINK https:/www.MedChemE/cathepsin-inhibitor-1.html 1Cat. No.: HY-103351 Cat. No.: HY-100231Cathepsin G Inhibitor I is a potent, selective,reversible, competitive, no

32、n-peptide inhibitor ofcathepsin G.Cathepsin inhibitor 1 (compound 25) is a potentand selective inhibitor of Cathepsin, with pIC s50of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2,CatS, CatK, and CatB, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Dat

33、a: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/Heptanamide,_N-_1-cyanocyclopropyl_-4,4-difluoro-2-_1S_-2,2,2-trifluoro-1-_4-fluorophenyl_ethylamino-,_2S_-.html Cathepsin HYPERLINK https:/www.MedChemE/Heptanamide,_N-_1-cyanocyclopropyl_-4,4-difluoro-2-_1S_-2,2,2-trifluoro-1-_4-flu

34、orophenyl_ethylamino-,_2S_-.html HYPERLINK https:/www.MedChemE/Heptanamide,_N-_1-cyanocyclopropyl_-4,4-difluoro-2-_1S_-2,2,2-trifluoro-1-_4-fluorophenyl_ethylamino-,_2S_-.html Inhibitor HYPERLINK https:/www.MedChemE/Heptanamide,_N-_1-cyanocyclopropyl_-4,4-difluoro-2-_1S_-2,2,2-trifluoro-1-_4-fluorop

35、henyl_ethylamino-,_2S_-.html HYPERLINK https:/www.MedChemE/Heptanamide,_N-_1-cyanocyclopropyl_-4,4-difluoro-2-_1S_-2,2,2-trifluoro-1-_4-fluorophenyl_ethylamino-,_2S_-.html 2 HYPERLINK https:/www.MedChemE/Heptanamide,_N-_1-cyanocyclopropyl_-4,4-difluoro-2-_1S_-2,2,2-trifluoro-1-_4-fluorophenyl_ethyla

36、mino-,_2S_-.html HYPERLINK https:/www.MedChemE/cathepsin-k-inhibitor-2.html Cathepsin HYPERLINK https:/www.MedChemE/cathepsin-k-inhibitor-2.html HYPERLINK https:/www.MedChemE/cathepsin-k-inhibitor-2.html K HYPERLINK https:/www.MedChemE/cathepsin-k-inhibitor-2.html HYPERLINK https:/www.MedChemE/cathe

37、psin-k-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/cathepsin-k-inhibitor-2.html HYPERLINK https:/www.MedChemE/cathepsin-k-inhibitor-2.html 2Cat. No.: HY-U00377 Cat. No.: HY-143714Cathepsin Inhibitor 2 is a potent Cathepsin Sinhibitor extracted from patent WO2009123623A1,has a K of 98%Cl

38、inical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cathepsin-l-in-2.html Cathepsin HYPERLINK https:/www.MedChemE/cathepsin-l-in-2.html HYPERLINK https:/www.MedChemE/cathepsin-l-in-2.html L-IN-2 HYPERLINK

39、 https:/www.MedChemE/cathepsin-l-in-2.html HYPERLINK https:/www.MedChemE/chymostatin.html Chymostatin(Z-Phe-Phe-FMK) Cat. No.: HY-115733Cat. No.: HY-P3042Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent andirreversible cathepsin L and cathepsin Binhibitor.Chymostatin is a potent cathepsin G inhibitor.Ch

40、ymostatin inhibits fungal growth when combinedwith other pepsin inhibitors. Chymostatin can beused for acute lung injury and pancreatitisresearch.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedC

41、hemE 3 HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor.html Cysteine HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor.html HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor.html Protease HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor.html HYPERLINK https:/www.Me

42、dChemE/Cysteine-Protease-inhibitor.html inhibitor HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor.html HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor-hydrochloride.html Cysteine HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor-hydrochloride.html HYPERLINK https:/www.Med

43、ChemE/Cysteine-Protease-inhibitor-hydrochloride.html Protease HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor-hydrochloride.html HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor-hydrochloride.html inhibitor HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor-hydrochloride.ht

44、ml HYPERLINK https:/www.MedChemE/Cysteine-Protease-inhibitor-hydrochloride.html hydrochlorideCat. No.: HY-17541 Cat. No.: HY-17541ACysteine Protease inhibitor is an inhibitor ofcysteine protease. IC50 & Target: CysteineProtease.Cysteine Protease inhibitor hydrochloride is aninhibitor of cysteine pro

45、tease. IC50 & Target:Cysteine Protease.Purity: 96.29%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 96.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cysteine-protease-inhibitor-2.html Cysteine HYPERLINK

46、 https:/www.MedChemE/cysteine-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/cysteine-protease-inhibitor-2.html protease HYPERLINK https:/www.MedChemE/cysteine-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/cysteine-protease-inhibitor-2.html inhibitor-2 HYPERLINK https:/www.MedChem

47、E/cysteine-protease-inhibitor-2.html HYPERLINK https:/www.MedChemE/Loxistatin_acid.html E HYPERLINK https:/www.MedChemE/Loxistatin_acid.html HYPERLINK https:/www.MedChemE/Loxistatin_acid.html 64cCat. No.: HY-21141 Cat. No.: HY-100227Cysteine protease inhibitor-2 is a cysteineprotease inhibitor extra

48、cted from patentUS20070032499A1, compound 12. Cysteine proteaseinhibitor-2 inhibits the cells growth of DCT116and PC3 cells with GI values of 6.5 M and 4.450M, respectively.E 64c is a derivative of naturally occurringepoxide inhibitor of cysteine proteases, aCalcium-activated neutral protease (CANP)

49、inhibitor and a very weak irreversible cathepsin Cinhibitor. E 64c exhibits entry-blocking effectfor MERS-CoV.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPER

50、LINK https:/www.MedChemE/E-64.html E-64(Proteinase inhibitor E 64) Cat. No.: HY-15282 HYPERLINK https:/www.MedChemE/gsk-2793660-1.html GSK-2793660Cat. No.: HY-112318AE-64 (Proteinase inhibitor E 64) is a potentirreversible inhibitor against general cysteineproteases IC50 papainwith of 9 nM for .GSK-

51、2793660 is an orally active and irreversibleinhibitor of Cathepsin C (CTSC). GSK-2793660 canbe used for the research of bronchiectasis.Purity: 99.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.66%Clinical Data: No Development ReportedSize: 5 mg, 10 mg,

52、 25 mg, 50 mg HYPERLINK https:/www.MedChemE/gsk-2793660.html GSK-2793660 HYPERLINK https:/www.MedChemE/gsk-2793660.html HYPERLINK https:/www.MedChemE/gsk-2793660.html free HYPERLINK https:/www.MedChemE/gsk-2793660.html HYPERLINK https:/www.MedChemE/gsk-2793660.html base HYPERLINK https:/www.MedChemE

53、/gsk-2793660.html HYPERLINK https:/www.MedChemE/jpm-oet.html JPM-OEtCat. No.: HY-112318 Cat. No.: HY-102087GSK-2793660 (free base) is an oral, irreversibleinhibitor of Cathepsin C (CTSC). GSK-2793660(free base) can be used for the research ofbronchiectasis.JPM-OEt is a broad spectrum cysteine cathep

54、sininhibitor. JPM-OEt binds covalently in the activesite, and irreversibly inhibits the cysteinecathepsin family. Antitumor activity.Purity: 98%Clinical Data: Phase 1Size: 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLI

55、NK https:/www.MedChemE/k777.html K777 HYPERLINK https:/www.MedChemE/k777.html HYPERLINK https:/www.MedChemE/l-006235.html L-006235Cat. No.: HY-119293(L-235) Cat. No.: HY-103352K777 is a potent, orally active and irreversiblecysteine protease inhibitor. K777 is also a potentCYP3A4 inhibitor with an I

56、C of 60 nM and a50selective CCR4 antagonist featuring the potentchemotaxis inhibition.Purity: 99.60%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgL-006235 (L-235) is a potent, selective,reversible and orally active inhibitor of cathepsinK, with an IC of 5 nM in bone re

57、sorption assay.50L-006235 shows selectivity for cathepsin K (K=0.2inM) over cathepsin B, cathepsin L, and cathepsin S(K=1, 6, and 47 M, respectively).iPurity: 99.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: s

58、alesMedChemE HYPERLINK https:/www.MedChemE/MK-0822.html L-873724 HYPERLINK https:/www.MedChemE/MK-0822.html HYPERLINK https:/www.MedChemE/Leupeptin-hemisulfate.html Leupeptin HYPERLINK https:/www.MedChemE/Leupeptin-hemisulfate.html HYPERLINK https:/www.MedChemE/Leupeptin-hemisulfate.html hemisulfate

59、Cat. No.: HY-50887 Cat. No.: HY-18234AL-873724 is a potent, orally bioavailable,selective and reversible non-basic cathepsin Kinhibitor, with IC s of 0.2, 178, 264, and 523950nM for cathepsin K, cathepsin S, cathepsin L,cathepsin B, respectively. L-873724 also exhibitsan IC of 0.5 nM for rabbit cath

60、epsin K.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgLeupeptin hemisulfate is a membrane-permeable thiolprotease inhibitor that inhibits Cathepsin B,Cathepsin H and Cathepsin L, and also impairsamphisome-lysosome fusion. Leupeptin hemisulfatealso exhibits anti-inflammatory effe