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 D and E FRET Substrate

Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D[1].

  • CAS Number: 839730-93-7
  • MF: C85H122N22O19
  • MW: 1756.014
  • Catalog: Cathepsin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ASPER-29

ASPER-29 is Asperphenamate HY-129578 analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC50 value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer[1].

  • CAS Number: 2630388-03-1
  • MF: C31H29BrN2O5S
  • MW: 621.54
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-Leu-Tyr-chloromethylketone

Z-Leu-Tyr-Chloromethylketone is a calpain inhibitor[1].

  • CAS Number: 56979-35-2
  • MF: C24H29ClN2O5
  • MW: 460.95000
  • Catalog: Cathepsin
  • Density: 1.231g/cm3
  • Boiling Point: 693.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 373.2ºC

GSK-2793660

GSK-2793660 is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis[1][2].

  • CAS Number: 1613458-70-0
  • MF: C20H27N3O3
  • MW: 357.45
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK-0822

L-873724 is a potent, orally bioavailable, selective and reversible[2] non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively[1]. L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption[2].

  • CAS Number: 603139-12-4
  • MF: C23H26F3N3O3S
  • MW: 481.53100
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Odanacatib(MK-0822)

Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.

  • CAS Number: 603139-19-1
  • MF: C25H27F4N3O3S
  • MW: 525.559
  • Catalog: Cathepsin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 681.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 366.0±31.5 °C

Z-Phe-Phe-diazomethylketone

Z-Phe-Phe-Diazomethylketone is a selective inhibitor of cathepsin L[1].

  • CAS Number: 65178-14-5
  • MF: C27H26N4O4
  • MW: 470.52000
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Suc-Val-Pro-Phe-pNA

Suc-Val-Pro-Phe-pNA is a substrate for cathepsin G and can be used to detect the activity of this enzyme[1].

  • CAS Number: 95192-11-3
  • MF: C29H35N5O8
  • MW: 581.61700
  • Catalog: Cathepsin
  • Density: 1.337±0.06 g/cm3 (20 °C, 760 mmHg)
  • Boiling Point: 971.6±65.0 °C (760 mmHg)
  • Melting Point: N/A
  • Flash Point: N/A

Cathepsin L inhibitor

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor[1][2].

  • CAS Number: 167498-29-5
  • MF: C26H26N2O5
  • MW: 446.49500
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CA 074 TFA

CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.

  • CAS Number: 134448-10-5
  • MF: C18H29N3O6
  • MW: 383.43900
  • Catalog: Cathepsin
  • Density: 1.267g/cm3
  • Boiling Point: 728.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 394.7ºC

Gü1303

Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen[1].

  • CAS Number: 1043922-53-7
  • MF: C20H22N4O3
  • MW: 366.41
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Petesicatib

Petesicatib is a cathepsin S inhibitor, used in research of immune diseases[1].

  • CAS Number: 1252637-35-6
  • MF: C25H23F6N5O4S
  • MW: 603.54
  • 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

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

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

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

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

MDL 27399

MDL 27399 is an inhibitor of human neutrophil cathepsin G (Ki = 7 μM). MDL 27399 can be used for research of inflammatory diseases[1].

  • CAS Number: 131374-22-6
  • MF: C26H36N4O8
  • MW: 532.58600
  • Catalog: Cathepsin
  • Density: 1.239g/cm3
  • Boiling Point: 840.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 462.2ºC

Z-Gly-Pro-Arg-AMC · HCl

Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsin K activity[1][2].

  • CAS Number: 201928-42-9
  • MF: C31H38ClN7O7
  • MW: 656.12900
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LmCPB-IN-1

LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7[1].

  • CAS Number: 2151025-98-6
  • MF: C18H30N6O2
  • MW: 362.47
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S130

S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux[1].

  • CAS Number: 1160852-22-1
  • MF: C24H25N3O2
  • MW: 387.47
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Leupeptin

Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].

  • CAS Number: 55123-66-5
  • MF: C40H78N12O12S
  • MW: 951.18600
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cathepsin Inhibitor 2

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.

  • CAS Number: 1017931-53-1
  • MF: C19H21F6N3O
  • MW: 421.38
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-Leu-Leu-Arg-AMC

Z-Leu-Leu-Arg-AMC is a peptide substrate of cathepsin S[1].

  • CAS Number: 90468-17-0
  • MF: C36H49N7O7
  • MW: 691.81700
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A