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

SID 26681509

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G[1].

  • CAS Number: 958772-66-2
  • MF: C27H33N5O5S
  • MW: 539.64600
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

calpeptin

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets[1]. Calpeptin is also an inhibitor of cathepsin K[2].

  • CAS Number: 117591-20-5
  • MF: C20H30N2O4
  • MW: 362.463
  • Catalog: Cathepsin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 550.7±45.0 °C at 760 mmHg
  • Melting Point: 60-75 °C
  • Flash Point: 286.8±28.7 °C

Z-FA-FMK

(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position[1][2].

  • CAS Number: 105637-38-5
  • MF: C21H23FN2O4
  • MW: 386.41700
  • 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

p-aminophenylmercuric acetate

p-Aminophenylmercuric acetate is an organomercurial activator of matrix metalloproteinases (MMP). P-Aminophenylmercuric acetate participates in the activation and inhibition of MMP-8 by attacking protein sulfhydryl or inducing cysteine switching reaction. p-Aminophenylmercuric acetate promotes the shedding of betacellulin precursor (pro-BTC). p-Aminophenylmercuric acetate influences the binding of agonists and antagonists to the opiate receptor[1][2][3].

  • CAS Number: 6283-24-5
  • MF: C8H9HgNO2
  • MW: 351.75
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 163-165 °C(lit.)
  • Flash Point: N/A

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

Z-LVG-CHN2

Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease[3].

  • CAS Number: 119670-30-3
  • MF: C22H31N5O5
  • MW: 445.51
  • Catalog: HSV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-WEHD-FMK

Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis[1][2][4].

  • CAS Number: 210345-00-9
  • MF: C37H42FN7O10
  • MW: 763.76900
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Cyanopyrimidine

2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos[1].

  • CAS Number: 14080-23-0
  • MF: C5H3N3
  • MW: 105.097
  • Catalog: Cathepsin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 250.7±23.0 °C at 760 mmHg
  • Melting Point: 40-44 °C(lit.)
  • Flash Point: 97.2±7.8 °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

Ac-Leu-Val-Lys-aldehyde

Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II[1].

  • CAS Number: 147600-40-6
  • MF: C19H36N4O4
  • MW: 384.51
  • Catalog: Cathepsin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 665.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 356.3±31.5 °C

Z-Phe-Phe-FMK

Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor[1][2].

  • CAS Number: 108005-94-3
  • MF: C27H27FN2O4
  • MW: 462.51
  • 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

Aurantiamide acetate

Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of  inflammatory diseases[1][2].

  • CAS Number: 56121-42-7
  • MF: C27H28N2O4
  • MW: 444.522
  • Catalog: Cathepsin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 716.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 386.9±32.9 °C

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

Atg4B-IN-2

Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer drugs via autophagy inhibition[1].

  • CAS Number: 2765008-88-4
  • MF: C21H30O3
  • MW: 330.46
  • Catalog: Autophagy
  • 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

CA-074 methyl ester

CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

  • CAS Number: 147859-80-1
  • MF: C19H31N3O6
  • MW: 397.46600
  • Catalog: Cathepsin
  • Density: N/A
  • 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

Cathepsin K inhibitor 3

Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies[1].

  • CAS Number: 1694638-70-4
  • MF: C30H31FN4O4S
  • MW: 562.65
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • 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