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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Z-Arg-Arg-pNA

Z-Arg-Arg-pNA is a substrate for cathepsin B and can be used to detect this enzyme activity[1].

  • CAS Number: 122630-71-1
  • MF: C26H36N10O6
  • MW: 584.63
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LHVS

LHVS is a potent, non-selective cysteine protease inhibitor[1]. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion[2].

  • CAS Number: 170111-28-1
  • MF: C28H37N3O5S
  • MW: 527.68
  • Catalog: Parasite
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH

H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that can serve as a substrate for cathepsin D, pepsin and pepsinogen. H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH has potential applications in biochemical analysis[1][2].

  • CAS Number: 90331-82-1
  • MF: C44H63N11O13
  • MW: 954.04
  • Catalog: Cathepsin
  • Density: 1.45g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ALLM

ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI)[1][2].

  • CAS Number: 110115-07-6
  • MF: C19H35N3O4S
  • MW: 401.564
  • Catalog: Cathepsin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 676.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 362.9±31.5 °C

Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 trifluoroacetate salt

Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a cathepsin D substrate, that can be used for cathepsin D FRET assay[1].

  • CAS Number: 400716-78-1
  • MF: C104H146N24O23S
  • MW: 2132.484
  • Catalog: Cathepsin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

Gü2602

Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen[1].

  • CAS Number: 1627094-88-5
  • MF: C16H22N4O3
  • MW: 318.37
  • Catalog: Cathepsin
  • Density: N/A
  • 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

Z-Phe-Ala-diazomethylketone

Z-Phe-Ala-diazomethylketone binds directly to Aβ42 monomers and small oligomers. Z-Phe-Ala-diazomethylketone inhibits the formation of Aβ42 dodecamers and inhibits Aβ42 fibril formation in the solution. Z-Phe-Ala-diazomethylketone has the potential for neurodegenerative disorders research[1].

  • CAS Number: 71732-53-1
  • MF: C21H22N4O4
  • MW: 394.42400
  • 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

Cathepsin K inhibitor 5

Cathepsin K inhibitor 5 is a potent Cathepsin K inhibitor[1].

  • CAS Number: 448945-62-8
  • MF: C35H51N7O8
  • MW: 697.82
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-ALPHA-CBZ-ARG-ARG 7-AMIDO-4-METHYLCOUMARIN HYDROCHLORIDE

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

  • CAS Number: 136132-67-7
  • MF: C30H40ClN9O6
  • MW: 658.14800
  • 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

Z-Asp-Glu-Val-Asp-chloromethylketone

Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro[1].

  • CAS Number: 250584-13-5
  • MF: C27H35ClN4O12
  • MW: 643.04
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • 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

Z-FG-NHO-BzOME

Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain[1].

  • CAS Number: 180313-86-4
  • MF: C27H27N3O7
  • MW: 505.52
  • 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

RKLLW-NH2

RKLLW-NH2 is a Cathepsin L inhibitor[1].

  • CAS Number: 289480-71-3
  • MF: C35H59N11O5
  • MW: 713.91
  • Catalog: Cathepsin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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

SSAA09E1

SSAA09E1 is a cathepsin L blocker (IC50: 5.33 μM).SSAA09E1 inhibits stages of viral entry. SSAA09E1 can be used for SARS-CoV infection research[1]

  • CAS Number: 433212-75-0
  • MF: C7H9N3S2
  • MW: 199.296
  • Catalog: SARS-CoV
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 333.0±34.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 155.2±25.7 °C

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

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

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-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