Cathepsin Inhibitor

Cathepsin L-IN-3 (Compound cat L inh. 7) TFA is selective a noncovalent cathepsin L inhibitor with a K_i of 4.3 nM.

Kgp-IN-1 hydrochloride is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.

CTSE Human Pre-designed siRNA Set A contains three designed siRNAs for CTSE gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cysteine Protease inhibitor hydrochloride, an inhibitor of Cysteine Protease, binds to acetylcholinesterase (AChE). Cysteine Protease inhibitor hydrochloride is applicable to the research of Alzheimer's disease.

CTSC Human Pre-designed siRNA Set A contains three designed siRNAs for CTSC gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

SNJ-1945 is an orally active, blood-brain barrier-penetrant Calpain inhibitor. SNJ-1945 inhibits Cathepsin L, Cathepsin B, and Ca²⁺ -independent proteases. SNJ-1945 suppresses ROS production and downregulates Cyclooxygenase-2 and Caspase-1. SNJ-1945 alleviates left ventricular systolic dysfunction, reduces cerebral ischemia-induced injury, and decreases the score of experimental autoimmune encephalomyelitis in mouse models. SNJ-1945 can be used in research related to post-cardiac arrest reperfusion injury, Parkinson's disease, multiple sclerosis, and proliferative retinopathy.

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.

Ctsd Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ctsd gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.

CTSB Human Pre-designed siRNA Set A contains three designed siRNAs for CTSB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

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

GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis.

SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC₅₀ of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows no inhibitory activity against cathepsin G.

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.

Ac-PLVE-FMK (Ac-Pro-Leu-Val-Glu(OMe)-CH2F), a tetrapeptidyl m-FMKs, is a Cats inhibitor. Ac-PLVE-FMK can be used for the research of cancer.

Z-Val-Val-Nle-diazomethylketone is a cathepsin S (CATS) inhibitor. Z-Val-Val-Nle-diazomethylketone significantly inhibits the IFNg-induced upregulation of the MHCII molecules HLA-DR and Ii-p33/35 with an increase of Ii-p10 protein level. Z-Val-Val-Nle-diazomethylketone can be used for dermatological diseases like psoriasis, atopic dermatitis and actinic keratosis research.

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

JNJ-10311795 (RWJ-355871), a potent dual inhibitor of neutrophil cathepsin G (K_i = 38 nM) and mast cell chymase (K_i = 2.3 nM), exhibits noteworthy antiinflammatory activity.

AZD5248 is an orally active, selective dipeptidyl peptidase 1 (cathepsin C) inhibitor, with IC₅₀ values of 1 nM and 17 nM against human CatC, 44 nM against human DPP1, and 67 nM against rat DPP1. It exhibits low clearance and high bioavailability in animal models. AZD5248 forms an irreversible covalent bond with the catalytic Cys234 residue of CatC, exerts reversible inhibition via its nitrile moiety, blocks CatC-dependent amyloid formation, and reduces the activation levels of neutrophil serine proteases in bone marrow and blood. AZD5248 reacts with aortic elastin aldehydes to form stable 4-imidazolinones, induces ultrastructural changes in aortic tissue, and has an α-amino acid-based backbone. AZD5248 reduces the severity of acute pancreatitis in mouse models. AZD5248 can be used in research on chronic obstructive pulmonary disease, acute pancreatitis, neurodegenerative diseases, lysosomal storage disorders, acute lung injury, cystic fibrosis, and neutrophil-mediated inflammatory diseases.

Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC₅₀: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC₅₀: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC₅₀: 50 nM).