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)

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.

Calpeptin is a potent, cell-permeable calpain inhibitor.

SPR39, a potent inhibitor of the SARS-CoV-2 main protease (Mpro), demonstrates inhibitory Ki values of 0.252 µM for SARS-CoV-2 Mpro, and 3.38 and 7.88 µM for human Cathepsin L (hCatL) and human Cathepsin B (hCatB) respectively. It exhibits antiviral properties and cytotoxicity.

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.

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.

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 .

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.

SPR38, a potent inhibitor of the SARS-CoV-2 main protease, exhibits a Ki value of 0.260 μM. Additionally, it effectively inhibits human cathepsin L (hCatL) and human cathepsin B (hCatB), displaying Ki values of 1.92 μM and 11.1 μM, respectively.

Acetyl-Calpastatin(184-210)(human) TFA, a potent, selective, and reversible calpain inhibitor, has Ki values of 0.2 nM for µ-calpain and 6 μM for cathepsin L, indicating high specificity and efficacy in enzyme inhibition [1] [2].

Ac-VLPE-FMK, a tetrapeptidyl mono-fluoromethyl ketone (m-FMK), inhibits Cathepsin B (Cat-B) and Cathepsin L (Cat-L) and is used in cancer aggressiveness research [1] [2].

Cathepsin C-IN-6 (compound 2), an E-64c-hydrazideas-derived inhibitor of cathepsin C, possesses anti-inflammatory properties and impedes neutrophil elastase activation, demonstrating potential efficacy in treating inflammatory diseases characterized by elevated neutrophil counts, such as chronic obstructive pulmonary disease (COPD) [1].