cathepsin inhibitor 2

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: <20 nM).

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.

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.

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

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

GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 is a bioactive dipeptide that can be used for the research of bronchiectasis [1] [2].

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

ALLM (Calpain inhibitor II), a potent calpain and cathepsin protease inhibitor, not only prevents neuronal cell death but also enhances chronic neurological function following spinal cord injury (SCI)[1][2].

CathepsinL-IN-5 (D6-3) is a potent inhibitor of Cathepsin L (CatL) with an IC50 value of 0.27 nM. It effectively blocks the function of CatL and significantly impedes the entry of SARS-CoV-2 pseudovirus into cells by inhibiting the cleavage of the spike protein. CathepsinL-IN-5 is applicable for research on infections.

SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 MPro with an IC50 of 11 nM. Additionally, this compound effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively.

DualCathepsinL/JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1/2/3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL/JAK-IN-1 is applicable in research on acute lung injury (ALI).

VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) and SARS-CoV-2 3CLpro (3CL-PR), with Ki values of 2.6 nM and 0.55 nM, respectively. It also exhibits activity against CoV-2, with an EC50 value of 1.25 μM.

SARS-CoV-2 3CLpro-IN-22 (Compound 17) is an inhibitor of cathepsin L (CTSL) with an IC50 value of 32.5 nM, useful in research related to the SARS-CoV-2 virus.

FGA146 is a selective inhibitor of Mpro and human Cathepsin L, with Ki values of 2.19 μM for Mal-Mpro, 0.96 μM for pET21-Mpro, and 0.87 μM for Cathepsin L. It exhibits antiviral activity against SARS-CoV-2.

SARS-CoV-2-IN-77 (compound 11e) is an inhibitor of cathepsin L and cathepsin S, with Ki values of 111 nM and 103 nM, respectively. It effectively inhibits SARS-CoV-2 in Calu-3 cells with an EC50 value of 38.4 nM and does not exhibit cytotoxicity.

Mpro/Cathepsin L-IN-1 (Compound 4d) is an inhibitor of SARS-CoV-2 Mpro and hCatL, with Ki values of 5.54 μM and 0.701 μM, respectively.

Mpro/Cathepsin L-IN-2 (Compound 1) is an irreversible dual inhibitor targeting the main protease of SARS-CoV-2 (Mpro, pIC50=8.61) and human cathepsin L (hCTSL, pIC50=7.64). Mpro/Cathepsin L-IN-2 shows potential for use in research related to COVID-19 and other coronavirus infections.

CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.1It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50= 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50= 5.33 μM) but not cathepsin B when used at a concentration of 20 μM. 1.()

(Rac)-Z-Phe-Phe-FMK (Cathepsin L-IN-2) is a cathepsin L inhibitor that inhibits the tendency of β-amyloid to induce apoptotic changes .

Calpeptin is a potent, cell-permeable calpain inhibitor.

SARS-CoV-2 Mpro-IN-4 is a dual inhibitor targeting Main Protease (M Pro) and Cathepsin L (CatL), with inhibition concentrations (IC50) of 900 nM and 60 nM, respectively. It effectively blocks SARS-CoV-2 replication in hACE2-expressing A549 cells, demonstrating antiviral activity with an IC50 value of 8.2 nM.

SARS-CoV-2 Mpro-IN-5 is a dual inhibitor targeting Main Protease (M Pro) and Cathepsin L (CatL) with IC50 values of 1800 nM and 145 nM, respectively. This compound demonstrates antiviral activity by inhibiting SARS-CoV-2 replication in hACE2 expressing A549 cells, with an IC50 value of 14.7 nM.