2. シグナル伝達
  3. Metabolic Enzyme/Protease
  4. Cathepsin
  5. Cathepsin L Isoform

Cathepsin L

Cathepsin L (CTSL) is a ubiquitously expressed lysosomal cysteine proteinase involved in lysosomal proteolysis, MHC class II antigen presentation, prohormone processing, and extracellular matrix remodeling[1]. Mechanistically, CTSL supports invariant chain degradation in cortical thymic epithelial cells and contributes to CD4+ T-cell selection in the thymus[2]. It also regulates positively selecting peptide ligands independently of invariant chain degradation, showing that CTSL affects thymic MHC class II presentation through more than one mechanism[3]. In skin models, CTSL deficiency causes periodic hair loss, epidermal hyperplasia, altered hair follicle morphogenesis, and disturbed hair follicle cycling[1]. Keratinocyte hyperproliferation in CTSL-knockout mice results from enhanced recycling of growth factors and receptors from endosomes to the plasma membrane[4]. Compared with related isoforms, human cathepsin V is highly homologous to cathepsin L, is expressed in human thymus and testis, and lacks a mouse orthologue[5]. In SARS-CoV-2 models, CTSL cleaves spike protein and enhances viral entry, while CTSL inhibition reduces pseudovirus infection in vitro and in vivo[6]. For experimental applications, small-molecule inhibitors and functional probes help define human CTSL mechanisms in specific cellular contexts[7].

製品番号 製品名 製品効果 純度
  • HY-15282
    E-64 Inhibitor 99.96%
    E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
  • HY-W010347
    L-Homocysteine Activator 98.0%
    L-Homocysteine, an amino acid, is a homocysteine that has L configuration. Homocysteine is an essential intermediate in normal mammalian metabolism of methionine. L-Homocysteine induces upregulation of Cathepsin V that mediates vascular endothelial inflammation in hyperhomocysteinaemia.
  • HY-128140
    Z-FY-CHO Inhibitor
    Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.
  • HY-103353
    SID 26681509 Inhibitor 99.16%
    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.
  • HY-142021
    Z-Leu-Arg-AMC Substrate 99.24%
    Z-Leu-Arg-AMC is a fluorogenic peptide substrate for cysteine proteases (e.g., Cathepsin) (Ex=350 nm，Em=460 nm). Z-Leu-Arg-AMC is preferentially cleaved by Cathepsin K and S under weakly acidic conditions, while its hydrolysis relies on residual Cathepsin S activity at neutral pH. Z-Leu-Arg-AMC serves as a substrate for recombinant Sphenophorus levis Cathepsin L, falcipain-2, falcipain-3, berghepain-2, knowlepain-2, vivapain-2, as well as falcipain-2 chimeras and constructs. It enables quantitative detection of cysteine protease activity in human inflammatory bronchoalveolar lavage fluid via fluorescence generation. Z-Leu-Arg-AMC can be used in research related to pulmonary inflammatory diseases and malaria.
  • HY-P10118A
    Cathepsin L-IN-3 TFA Inhibitor 98.18%
    Cathepsin L-IN-3 (Compound cat L inh. 7) TFA is selective a noncovalent cathepsin L inhibitor with a Ki of 4.3 nM.
  • HY-180799
    Cathepsin L-IN-6 Inhibitor
    Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC50 of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.
  • HY-182269
    Cathepsin-IN-5 Inhibitor
    Cathepsin-IN-5 is a cathepsin inhibitor with IC50 values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma.
  • HY-15100
    Balicatib Inhibitor 98.25%
    Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.
  • HY-P0109A
    Z-FA-FMK Inhibitor 99.14%
    Z-FA-FMK ((1S)-Z-FA-FMK) is a potent Cathepsin B and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host.
  • HY-128971
    LHVS Inhibitor 98.15%
    LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM.
  • HY-115733
    Cathepsin L-IN-2 Inhibitor 98.02%
    Cathepsin L-IN-2 ((Rac)-Z-Phe-Phe-FMK) is an isomer of the Cathepsin L inhibitor Z-Phe-Phe-FMK (HY-141867), with an IC50 of 15 μM for cathepsin L. Z-Phe-Phe-FMK irreversibly blocks the proteolytic function of cathepsins by covalently binding to the cysteine residues in the active center of the enzyme. Cathepsin L-IN-2 and Z-Phe-Phe-FMK can be used to study neurodegenerative diseases (such as GRN-related frontotemporal dementia) and cancer invasion and metastasis.
  • HY-141867
    Z-FF-FMK Inhibitor
    Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease.
  • HY-N2905
    Aurantiamide acetate Inhibitor 99.85%
    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.
  • HY-10294
    Relacatib Inhibitor 99.99%
    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.
  • HY-N4289
    3-Epiursolic Acid Inhibitor 99.77%
    3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B.
  • HY-152204
    Cathepsin L/S-IN-1 Inhibitor 99.89%
    Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC50s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells.
  • HY-138208
    Z-Phe-Tyr(tBu)-diazomethylketone Inhibitor ≥99.0%
    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.
  • HY-N6674
    Diazepinomicin Inhibitor 98.04%
    Diazepinomicin (ECO-4601) is an anticancer and antibacterial agent. Diazepinomicin can be produced by a Micromonospora strain. Diazepinomicin induces Apoptosis. Diazepinomicin inhibits the proteases Rhodesain and Cathepsin L at an IC50 of 70-90 μM. Diazepinomicin possesses anti-inflammatory and anti-tumor activity. Diazepinomicin has demonstrated activity against hepatocellular carcinoma. Diazepinomicin shows antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 μM. Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL.
  • HY-137392
    Cathepsin L-IN-4 98.5%
    Cathepsin L-IN-4 is an inhibitor of cathepsin L with IC50 at nanomolar concentrations.
製品番号 製品名 / Synonyms Species Source