Cathepsins are proteases (enzymes that degrades proteins) found in all animals as well as other organisms. The cathepsin family of proteolytic enzymes contains several diverse classes of proteases. Most of the members become activated at the low pH found in lysosomes. The activity of this family lies almost entirely within those organelles. Cathepsins have a vital role in mammalian cellular turnover, e.g. bone resorption. They degrade polypeptides and are distinguished by their substratespecificities. Classification: Cathepsin A, Cathepsin B, Cathepsin C, Cathepsin D, Cathepsin E, Cathepsin F, Cathepsin G, Cathepsin H, Cathepsin K, Cathepsin L1, Cathepsin L2, Cathepsin O, Cathepsin S, Cathepsin W, Cathepsin Z. Most cathepsins are lysosomal and each is involved in cellular metabolism, participating in various events such as peptide biosynthesis and protein degradation. Cathepsins may also cleave some protein precursors, thereby releasing regulatory peptides.


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Cathepsin K inhibitor 2

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78)[1].

  • CAS Number: 2672478-52-1
  • MF: C30H33F4N5O3
  • MW: 587.61
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Asperphenamate

Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].

  • CAS Number: 63631-36-7
  • MF: C32H30N2O4
  • MW: 506.59200
  • Catalog: Autophagy
  • Density: 1.198g/cm3
  • Boiling Point: 774.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 422.1ºC

E-64c

E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor.

  • CAS Number: 76684-89-4
  • MF: C15H26N2O5
  • MW: 314.377
  • Catalog: Cathepsin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 596.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 314.5±30.1 °C

N-ethylmaleimide

N-Ethylmaleimide (NEM) is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2].

  • CAS Number: 128-53-0
  • MF: C6H7NO2
  • MW: 125.13
  • Catalog: Cathepsin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 210.0±9.0 °C at 760 mmHg
  • Melting Point: 43-46 °C(lit.)
  • Flash Point: 73.3±0.0 °C

VBY-825

VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.IC50 value: Target: 130/250/250/330/2.3/4.7 nM(Ki for cathepsin S/L/ZV/Bhumanized-rabbit cathepsin K/cathepsin F) [1]VBY-825 is a potent inhibitor of the assayed cathepsins and its potency against at least one cathepsin, cathepsin S, extends across species relevant for pharmacology studies, specifically mouse. 10 mg/kg/day dose of VBY-825 achieves a trough plasma concentration >200nM, which is well above that required for full inhibition of the intracellular activity of cathepsins B, F, K, L, S and V in both mouse and human cell lines.

  • CAS Number: 1310340-58-9
  • MF: C23H29F4N3O5S
  • MW: 535.55200
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dihydroxythiobinupharidine

6,6′-Dihydroxythiobinupharidine is a cysteine proteases inhibitor. 6,6′-Dihydroxythiobinupharidine can enhance DNA cleavage mediated by human topoisomerase IIα and IIβ ~8-fold and ~3-fold, respectively[1][2].

  • CAS Number: 30343-70-5
  • MF: C30H42N2O4S
  • MW: 526.73
  • Catalog: Cathepsin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 667.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 357.4±31.5 °C

4-Biphenylac-Cys(Me)-D-Arg-Phe-(2-phenylethyl)amide

Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.

  • CAS Number: 478164-48-6
  • MF: C41H49N7O4S
  • MW: 735.93700
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JPM-OEt

JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity[1][2].

  • CAS Number: 262381-84-0
  • MF: C20H28N2O6
  • MW: 392.44600
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-Gly-Gly-Tyr-Arg-OH

Papain inhibitor (Glycylglycyl-L-tyrosyl-L-arginine) acts as an effective competitive inhibitor to papain, with a Ki of 9 μM at pH 6.2[1].

  • CAS Number: 70195-20-9
  • MF: C19H29N7O6
  • MW: 451.48
  • Catalog: Cathepsin
  • Density: 1.49g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-Arg-Arg-AMC hydrochloride salt

Arg-Arg-AMC is a highly selective substrate of Cathepsin B. Arg-Arg-AMC can be used to cathepsin B activity assay in cancer cells, while cathepsin B is assocaited with cell invasive and metastatic phenotype in numerous types of cancer[1].

  • CAS Number: 263843-55-6
  • MF: C22H33N9O4
  • MW: 487.56
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SQ 32602

SQ 32602 is a cathepsin E inhibitor.

  • CAS Number: 125399-14-6
  • MF: C32H52N3O7P
  • MW: 621.756
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KGP-94

KGP-94 is a potent, selective cathepsin L inhibitor with IC50 of 189 nM, shows no significant inhibitory effect on cathepsin B (IC50>10 uM); significantly decreases the activity of cathepsin L toward human type I collagen, and impeds both migration and invasion of MDA-MB-231 human breast cancer cells; shows tumor growth retardation in a C3H mouse mammary carcinoma model.

  • CAS Number: 1131456-28-4
  • MF: C14H12BrN3OS
  • MW: 350.234
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-FG-NHO-Bz

Z-FG-NHO-Bz is a selective cathepsin inhibitor[1].

  • CAS Number: 118292-22-1
  • MF: C26H25N3O6
  • MW: 475.49
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ONO-5334

A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively; shows less or no potentcy for human cathepsin S/L/B/C (Ki=0.83/1.7/32/2500 nM); inhibits human osteoclasts bone resorption in vitro at a concentration more than 100 fold lower than that of alendronate; reduces plasma calcium level increased by PTHrP in thyroparathyroidectomized rats, decreases serum and urine C-telopeptide of type I collagen level. Osteoporosis Phase 2 Discontinued

  • CAS Number: 868273-90-9
  • MF: C21H34N4O4S
  • MW: 438.584
  • Catalog: Cathepsin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-Arg-Arg-AMC hydrochloride salt

Z-Arg-Arg-AMC is a selective substrate of cathepsin B[1].

  • CAS Number: 88937-61-5
  • MF: C30H39N9O6
  • MW: 621.68700
  • Catalog: Cathepsin
  • Density: 1.41g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

chymostatin

Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research[1].

  • CAS Number: 9076-44-2
  • MF: C31H41N7O6
  • MW: 607.701
  • Catalog: Cathepsin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 276-278℃
  • Flash Point: N/A

Papain

Papain is a cysteine protease of the peptidase C1 family, which is used in food, pharmaceutical, textile, and cosmetic industries.

  • CAS Number: 9001-73-4
  • MF: C19H29N7O6
  • MW: 451.477
  • Catalog: Cathepsin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: 29 °C

Calpain-1 (pig)

Calpain-1 (pig) (μ-Calpain) is an intracellular Ca2+-regulated cysteine protease. Calpain-1 (pig) exhibits neuroprotective effect[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK-0674

MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S. MK-0674 exhibits long half-lives in rats, rabbits and rhesus monkeys[1].

  • CAS Number: 887781-62-6
  • MF: C26H27F6N3O2
  • MW: 527.50200
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Leupeptin hemisulfate salt

Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor.

  • CAS Number: 103476-89-7
  • MF: C20H38N6O4.1/2H2SO4
  • MW: 475.59
  • Catalog: Peptides
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Epiursolic Acid

3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B[1].

  • CAS Number: 989-30-0
  • MF: C30H48O3
  • MW: 456.700
  • Catalog: Cathepsin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 556.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 304.7±26.6 °C

K777

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively[1][2][3].

  • CAS Number: 233277-99-1
  • MF: C32H38N4O4S
  • MW: 574.73
  • Catalog: CCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cathepsin L inhibitor III

Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection[1][2].

  • CAS Number: 114014-15-2
  • MF: C31H34N4O5
  • MW: 542.63
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Relacatib

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo[1][2].

  • CAS Number: 362505-84-8
  • MF: C27H32N4O6S
  • MW: 540.63100
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cathepsin Inhibitor 1

Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively[1].

  • CAS Number: 225120-65-0
  • MF: C20H24ClN5O2
  • MW: 401.89000
  • Catalog: Cathepsin
  • Density: 1.23±0.1 g/cm3 (20 ºC 760 Torr)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY 3000328

LY 3000328 is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.

  • CAS Number: 1373215-15-6
  • MF: C25H29FN4O5
  • MW: 484.520
  • Catalog: Cathepsin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 701.6±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 378.1±32.9 °C

Cysteine protease inhibitor-2

Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively[1].

  • CAS Number: 612048-23-4
  • MF: C13H5N5O
  • MW: 247.212
  • Catalog: Cathepsin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 597.2±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 315.0±30.1 °C

Cathepsin X-IN-1

Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic[1].

  • CAS Number: 2418577-51-0
  • MF: C15H13N3O3S
  • MW: 315.35
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NA-CBZ-ARG-ARG 4-METHOXY-B-NAPHTHYLAMIDE

Z-Arg-Arg-4MβNA triacetate is a cathepsin B-specific substrate and can produce fluorescent end product 4MβNA (λex = 355 nm, λem = 430 nm)[1][2].

  • CAS Number: 100900-19-4
  • MF: C33H45N9O7
  • MW: 679.76600
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E-64

E-64 is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.

  • CAS Number: 66701-25-5
  • MF: C15H27N5O5
  • MW: 357.405
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 182ºC
  • Flash Point: N/A