hepsin

Hepln-13 is a hepsin inhibitor that acts by hindering prostate cancer bone metastasis.

SRI 31215 TFA, a small molecule that acts as a triplex inhibitor of matriptase, hepsin and HGFA and mimics the activity of HAI-1/2, endogenous inhibitors of HGF activation with IC50s of 0.69 μM, 0.65 μM, 0.3 μM,

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

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.

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).

Cathepsin Inhibitor 4 (Compound 45) is a selective inhibitor of Cathepsin S, with a Ki value of 0.04 nM.

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.

CathepsinK-IN-8 (cxample 6-60) is an inhibitor of cathepsin K, which is useful for researching inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, and tumors.

CathepsinK-IN-9 is a selective, potent, and orally active Cathepsin K inhibitor with an IC50 of 6.2 nM. It exhibits an IC50 greater than 10000 nM against cathepsins B, L, and S, demonstrating over 1600-fold selectivity. CathepsinK-IN-9 also displays excellent safety and metabolic stability, making it suitable for osteoporosis research.

CathepsinL-IN-6 (Compound 6a) is a selective inhibitor of cathepsin L, with an IC50 of 0.021 μM. It inhibits cathepsin L by directly binding to it. Additionally, CathepsinL-IN-6 suppresses the expression of IL-6 and IL-8 and exhibits significant anti-inflammatory activity. This compound is applicable in research related to acute lung injury.

CathepsinC-IN-7 (Page 68) is an inhibitor of cathepsin C. It is applicable for research on primary cancers and cancer metastasis.

Mca-GKPILFFRL-Dpa-r-amide, FRET substrate for cathepsin D and E. Also cleaved by napsin A.

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E but not for B, H, or L. Cathepsin D and E FRET Substrate acetate can be used in mechanistic studies on cathepsins D and E studies.

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate selectively cleaved by cathepsins D and E at the Phe-Phe amide bond, demonstrating no activity towards cathepsins B, H, or L. This specificity renders it essential for routine assays and mechanistic studies focusing on cathepsins E and D[1].

Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor (IC50 = 7.13 μM) that reduces PC-3 cell migration with low cytotoxicity [1].

Cathepsin C-IN-5 (compound SF38) is a potent, selective, and orally active Cathepsin C inhibitor with an IC50 of 59.9 nM for Cat C, and significantly lower potency against Cat L (4.26 µM), Cat S, Cat B, and Cat K (all >5 µM). It reduces Cat C activity in bone marrow and blood, diminishes NSPs activation, and exhibits anti-inflammatory activity [1].

Cathepsin C-IN-4 is a potent inhibitor (IC50: 65.6 nM) of histone C. Cathepsin C-IN-4 inhibits THP-1 cells (IC50: 203.4 nM) and U937 cells (IC50: 177.6 nM).

Cathepsin C-IN-3 is a potent inhibitor of histone C (IC50: 61.79 nM) and also inhibits THP-1 cells (IC50: 101.5 nM) and U937 cells (IC50: 86.5 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.

Cathepsin K Inhibitor 3, exhibiting an IC50 value of 0.5 nM, is a highly selective inhibitor of cathepsin K, featuring a favorable pharmacokinetic profile. It holds potential for use in studies of osteoarthritis (OA).

Cathepsin L/S-IN-1, a dual inhibitor targeting Cathepsin L and Cathepsin S, exhibits potent and selective inhibition with IC50 values of 4.10 μM and 1.79 μM, respectively. Demonstrating significant antimetastatic and invasive effects, it effectively impacts pancreatic cancer BxPC-3 and PANC-1 cells.

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].