cysteine protease inhibitor

Cysteine protease inhibitors are inhibitors of cysteine proteases. Target: Cysteine Protease

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

Cysteine Protease inhibitor hydrochloride is a cysteine protease inhibitor.

Cysteine protease inhibitor-3 (Compound 15), a cysteine protease inhibitor, exhibits anti-plasmodial activity by effectively inhibiting Pf3D7 (IC50 = 0.74 μM), PfW2 (IC50 = 1.05 μM), PfFP2 (IC50 = 3.5 μM), and PfFP3 (IC50 = 4.9 μM), demonstrating efficacy against both drug-sensitive and drug-resistant parasites [1].

TAPI-2 is a broad-spectrum inhibitor of MMP (IC50: 20 μM), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM).

Hepatitis Virus C NS3 Protease Inhibitor 2, a peptide inhibitor derived from a product targeting the NS3 protease of the hepatitis C virus (HCV), exhibits inhibitory activity with a Ki value of 41 nM.

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

2-Cyanopyrimidine (m-Hydroxyphenylpropionic acid) is inhibitor of cathepsin K(IC50 : 170 nM)

BACE-IN-1 acetate (BACE-IN-1 acetate (350228-37-4，Free base)) has been used as β-site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) inhibitor in BACE1 inhibitor assay. β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1), an aspartic protease belongs to the protease family of enzymes comprises of six luminal cysteine residues. These residues help in the formation of three intermolecular disulfide bonds and N-linked glycosylation sites.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.

E-64 (Proteinase inhibitor E 64) is an irreversible and specific inhibitor of cysteine proteases, exhibiting an IC50 of 9 nM for papain.

Leupeptin is a competitive protease inhibitor produced by actinomycetes. Leupeptin can inhibit cysteine, serine and threonine peptidases. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine p

E 64c (EP 475) , a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.

NSC 185058, an inhibitor of ATG4B (a major cysteine protease), can also attenuate autophagic activity.

MDL-28170 (Calpain Inhibitor III) is a cysteine protease.

PF-00835231 is a CoV-2 cysteine 3C-like protease (3CLpro) inhibitor, with IC50s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CLpro, respectively. PF-00835231 is the active compound of the first anti-3CLpro regimen in clinical trials.

KGP94 is an inhibitor of cysteine protease Cathepsin L(CTSL).

WRR-483, an analogue of K-11777, is a potent and selective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777. WRR-483 demonstrates good potency against cruzain with sensitivity to pH conditions and high efficacy in the cell culture assay. Furthermore, WRR-483 also eradicates parasite infection in a mouse model of acute Chagas' disease. WRR-483 binds covalently to the active site cysteine of the protease in a similar manner as other vinyl sulfone-based inhibitors. WRR-483 has potential to be developed as a treatment for Chagas' disease.

Calpain Inhibitor-1 (compound 36) is a highly potent and selective inhibitor of Calpain 1 (Cal1), a cysteine protease, with an IC50 value of 100 nM and a Ki value of 2.89 μM.

LmCPB-IN-1 (compound 35) is a highly effective and reversible covalent inhibitor of Leishmania mexicana cysteine protease B (LmCPB), exhibiting a strong binding affinity with a pK i value of 9.7 [1].

A-933548 is a potent Calpain inhibitor. A-933548 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.

APC-3316 tosylate is a vinyl sulfone cysteine protease inhibitor and selective CCR4 antagonist.

APC-3316 hydrochloride is a vinyl sulfone cysteine protease inhibitor and selective CCR4 antagonist.

Z-L(D-Val)G-CHN2, an isoform of Z-LVG-CHN2, serves as a cell-permeable and irreversible inhibitor of cysteine proteinase. This tripeptide derivative emulates a segment of the human cysteine proteinase-binding center and demonstrates selective antiviral activity, inhibiting herpes simplex virus (HSV) yet exhibiting negligible impact on poliovirus replication. Notably, Z-LVG-CHN2 effectively impedes SARS-CoV-2 replication with an EC50 value of 190 nM by targeting the SARS-CoV-2 3CL protease [3].

Rupintrivirvr (AG7088) is a selective rhinovirus (HRV) 3C cysteine protease mimetic peptide inhibitor with antiviral and immunomodulatory activities.Rupintrivirvr inhibits the replication of EV71 and EV-D68, and may be useful for the study of viral infections.

3CPLro-IN-1 (compound A17) is a potent, orally active inhibitor of SARS-CoV-2 3-Chymotrypsin-like cysteine protease (3CLpro) with an IC50 of 5.65 μM, making it an attractive drug target against COVID-19 and also considered an antitumor agent-51.

Insulin-degrading enzyme (IDE) is a thiol-sensitive zinc-metallopeptidase that acts as the major insulin-degrading protease in vivo, mediating the termination of insulin signaling. [1] In addition to regulating insulin action in diabetes pathogenesis, IDE plays a role in Varicella-Zoster virus infection and degradation of amyloid-β, a peptide implicated in Alzheimer's disease. ML-345 is a small molecule inhibitor that selectively targets cysteine819 in IDE with an EC50 value of 188 nM. [2] It demonstrates 10-fold selectivity for IDE over a panel of enzymes with reactive cysteine residues.[2] Reference：[1]. Maianti, J.P., McFedries, A., Foda, Z.H., et al. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature 511(7507), 94-98 (2014).[2]. Bannister, T.D., Wang, H., Abdul-Hay, S.O., et al. ML345, a small-molecule inhibitor of the insulin-degrading enzyme (IDE). 1 R03 DA024888-01 (MLSCN cycle 6), 1-41 (2014).

SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a highly potent inhibitor specifically designed to target and inhibit the activity of SARS-CoV-2 3CL pro, a cysteine protease found in the main coronaviruses. This enzyme is a promising target for antiviral drug development, positioning SARS-CoV-2 3CLpro-IN-1 as significant for advancing research in infectious diseases [1].

SIC5-6 is a potent inhibitor of Separase, a substantial cysteine protease implicated in critical cellular processes such as chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, as well as spindle stabilization and elongation. Given its overexpression in many solid cancers, Separase presents an attractive target for chemotherapy [1].

Z-LVG, an irreversible cysteine protease inhibitor and a tripeptide derivative of cystatin C, serves as an inhibitor of viral replication and is utilized in research on viral diseases [1].

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K, a cysteine protease expressed under the control of the CTSK gene, which is closely related to osteoporosis and hydrolyses collagen. Cathepsin K inhibitor 2 has shown potential in osteoarthritis.

NVP-ABJ688 is the cysteine protease cathepsin K inhibitor.

A-953227 is a highly effective and selective inhibitor of calpain. A-953227 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.

3CPLro-IN-2 is a potent, orally active inhibitor of SARS-CoV-2 3CLpro (IC50: 1.55 μM, Ki: 6.09 μM). 3-Chymotrypsin-like cysteine protease (3CLpro) is an essential protein for viral replication and is a potential drug target against COVID-19.

Z-FG-NHO-BzOME is a chemical compound that functions as a cysteine protease inhibitor, selectively targeting and inhibiting cathepsin B, cathepsin L, cathepsin S, and papain [1].

Leupeptin is a naturally occurring protease inhibitor that can inhibit cysteine, serine and threonine peptidases. Leupeptin is an organic compound produced by actinomycetes. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine proteinases (papain, cathepsin B (Ki = 4.1 nM), endoproteinase Lys-C). It does not inhibit α-chymotrypsin or thrombin. Leupeptin is a competitive transition state inhibitor and its inhibition may be relieved by an excess of substrate.

TS-24 is an inhibitor of the cysteine protease histatin S (CTSS).TS-24 promotes BRCA1-mediated apoptosis and shows radiosensitization in a TNBC xenograft mouse model.

Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) acts as a cysteine protease inhibitor and has demonstrated efficacy in blocking SARS infection, while also providing protection to mice when challenged with T. crassiceps [1] [2].

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

BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1].

S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux.