Proteases/Proteasome

NS5A-IN-3 is a potent NS5A inhibitor with high efficacy against HCV 1b, good activity on 3a, and strong metabolic stability; superior to daclatasvir.

NS5A-IN-2, a potent inhibitor, is highly effective against HCV 1b and shows increased activity for GT 3a with good metabolic stability.

TP0556351: potent MMP2 inhibitor with 0.2 nM IC50, reduces collagen in pulmonary fibrosis mice.

ONO-4817 suppresses MMPs, limiting plaque progression and aortic hyperplasia in hyperlipidemic rabbits.

GS-6620 is a HCV nonstructural protein 5B (NS5B) inhibitor.

Ro 32-7315 is a selective inhibitor of ADAM17.

NCI-B16 is a small-molecule RNA binder that inhibits HCV (hepatitis C virus) replication [1].

Berotralstat HCl is a selective plasma kallikrein inhibitor, reducing pain and swelling in HAE by blocking bradykinin release.

Kallikrein-IN-2 (compound 1) is an inhibitor of the kinin-releasing enzyme Kallikrein.

Proteasome-IN-4, a potent non-covalent inhibitor (IC50=8.39nM), halts cancer cell growth, useful for oncology studies.

Cathepsin K inhibitor 3: Selective, IC50 of 0.5 nM, good pharmacokinetics, potential for OA research.

MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively).

Ravidasvir, also known as PPI-668 and ASC16, is a second-generation, orally active, potent and selective HCV NS5A protein inhibitor.

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

Atecegatran Metoxil (AZD0837), an oral thrombin inhibitor in development for stroke prevention in atrial fibrillation, is well-tolerated with favorable PK.

Cyclotheonellazole A inhibits elastase (IC50=0.034nM) & chymotrypsin (IC50=0.62nM), a natural macrocyclic peptide.

Inogatran is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of venous and arterial thrombotic diseases.

LY52 is a matrix metalloproteinase-2 inhibitor. It acts by suppressing tumor invasion and metastasis.

MMP-7-IN-2 acts as a selective and potent MMP7 inhibitor and can be used to study inflammatory responses and vascular-related diseases.

KCC009 is a potent and selective Transglutaminase 2 Inhibitor.

JTK-853: novel non-nucleoside HCV polymerase inhibitor with strong antiviral activity (EC50: 0.38 μM genotype 1a, 0.035 μM 1b).

PTC725 is a selective HCV 1b replicons inhibitor. It has been shown to target the nonstructural protein 4B.

MK-3281: Oral, potent HCV NS5B inhibitor with promising properties and efficacy in replication trials, suitable for clinical use.

Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).

Z-PDLDA-NHOH is a potent, specific vertebrate collagenase inhibitor [1].

Petesicatib is an inhibitor of cathepsin S. Petesicatib used in the research of immune diseases.

MMP13-IN-3 is an oral, selective MMP-13 inhibitor with IC50 of 1 nM, >1000x selective, for osteoarthritis treatment.

FK706, a human neutrophil elastase inhibitor (IC50: 83 nM, Ki: 4.2 nM), also blocks mouse and porcine elastases. Anti-inflammatory.

XL-784 is a selective MMP inhibitor with low IC50s for MMP-1,2,3,8,9,13, modulating extracellular matrix remodeling, tumor invasion, and metastasis in cancer.

GSK-2485852, a NS5B inhibitor, is used potentially for treatment of HCV infection.

XL-784 free base selectively inhibits MMPs with IC50: MMP-1 (1.9µM), MMP-2 (0.81nM), MMP-3 (120nM), MMP-8 (10.8nM), MMP-9 (18nM), MMP-13 (0.56nM).

MDL-101146, (R)- is an effective orally active inhibitor of human neutrophil elastase.

SSR69071: selective neutrophil elastase inhibitor, stronger for humans (Ki=0.0168 nM), may treat COPD, asthma, and reduce heart injury.

NK3201, a specific chymase inhibitor, suppresses bleomycin-induced pulmonary fibrosis in hamsters.

Phe-Pro-Ala-pNA is a chromogenic substrate utilized for assessing tripeptidyl peptidase activity.

DS-1040 Tosylate is a thrombin-activated fibrinolysis inhibitor (TAFI) inhibitor and a fibrinolysis enhancer, used for researching thromboembolic diseases.

MDL 27324 is an inhibitor of human neutrophil elastase.

BAY-678: Oral selective human neutrophil elastase inhibitor; IC50: 20 nM; SGC-approved chemical probe.

Z-FG-NHO-BzOME is a chemical compound functioning as a cysteine protease inhibitor, selectively targeting and inhibiting cathepsin B, cathepsin L, cathepsin S,

KB-R7785 is a novel ADAM12/MMP inhibitor improving heart function and insulin sensitivity by blocking HB-EGF and TNF-alpha.

MDL 101146 is an orally active neutrophil elastase inhibitor.

O-Benzoyl hydroxylamine exhibits properties as a dipeptidyl peptidase-IV (DPP-IV) inhibitor and demonstrates antidiabetic effects[1].

Neurodegenerative Disorder-Targeting Compound 1 is an inhibitor of calpain [1].

MMP-145 is used as a protease inhibitor.

BMS-189664 is an inhibitor of thrombin.

MMP-7-IN-3 (compound 15) is a potent and selective MMP-7 inhibitor, inhibiting renal fibrosis in a unilateral ureteral obstruction mouse model.

Matrix metalloproteinase-3 (MMP-3), also known as stromelysin-1, is a critical enzyme involved in tissue remodeling and repair through its role in degrading extracellular matrix proteins, facilitating cell migration. This enzyme has been implicated in various physiological processes including vascular remodeling associated with aneurysm formation, wound healing, the progression of atherosclerosis, and tumor initiation. MMP-3 inhibitor VIII, a cell-permeable sulfonamide-based hydroxamic acid, effectively inhibits MMP-3 by binding to its active site (Ki = 23 nM), thus blocking its enzymatic activity. Additionally, this inhibitor has been demonstrated to suppress the activity of mouse macrophage metalloelastase MME/MMP-12, with an IC50 value of 13 nM, highlighting its potential utility in research on tissue remodeling and disease processes involving MMPs.

Ro 31-9790 is a synthetic inhibitor of metalloproteinase (MMP).

Dim16, a dual inhibitor of PCSK9/HMG-CoAR, demonstrates potent activity with an IC50 of 19 nM against PCSK9 and significantly impedes PCSK9-LDLR interaction

Mergetpa, a carboxypeptidase inhibitor, impedes the conversion of kinins and B2 receptor antagonists into metabolites devoid of the C-terminal arginine [1].

HCV-IN-43 (compound 2), an HCV NS5B protein inhibitor, efficiently inhibits HCV virus replication and is utilized in the study of HCV infection [1].

LU-002i is a selective inhibitor targeting the human proteasome subunits β2c and β2i, demonstrating an inhibitory concentration (IC50) of 220 nM for β2i [1].

Beclabuvir (BMS-791325) is an HCV inhibitor targeting NS5B polymerase with sub-28 nM potency for genotypes 1, 3, 4, 5.

Paltimatrectinib (PBI-200) is a tyrosine kinase inhibitor with anticancer activity, and is used in the study of bladder, breast, and colorectal cancers.

Proteasome-IN-5, also known as compound 5, acts as a proteasome inhibitor [1].

M867 is a selective, reversible caspase-3 inhibitor, possessing an IC50 of 1.4 nM and a Ki value of 0.7 nM, demonstrating anti-apoptotic activity [1].

Proteasome β2c/i-IN-1 (compound 37) serves as a selective inhibitor targeting the β2c and β2i subunits of the human proteasome [1].

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7

MMP3 inhibitor 1 is a potent and highly selective inhibitor of MMP-3 (IC50 of 1 nM).

ASP8497 is a potent DPP-IV inhibitor enhancing GLP-1, used for type 2 diabetes and glucose intolerance.

LONP1-IN-2: Potent LONP1 inhibitor, IC50=0.187μM; weak on 20S proteasome (>10μM); for cancer research.

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

Cardanol diene: phenol in cashew shells; anti-tyrosinase (IC50=52.5μM); used to make anti-E. coli biofilm complexes.

BMS-538305 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP-IV).

AZD-9819 is a neutrophil elastase (HNE) inhibitor applicable for research into chronic obstructive pulmonary disease (COPD).

(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor.

MMP-9-IN-8 (Compound 3), an MMP-9 inhibitor, exhibits inhibitory activities of 42.16% at 10 μM and 58.28% at 50 μM.

LU-005i is a powerful inhibitor targeting the β5i subunit of immunoproteasomes, displaying a high potency with an IC 50 value of 6.6 nM, and exhibits selectivity by preferring β5i over the β5c subunit, which has an IC 50 value of 287 nM [1].

Collagen proline hydroxylase inhibitor-1 具有抗纤维增生活性。

Nesbuvir: HCV NS5B polymerase inhibitor, IC50 9 nM against HCV 1b replicon in liver cancer cells.

MK-0674 is a cathepsin K inhibitor (IC50: 0.4 nM) that inhibits Cat B, Cat F, Cat L, and Cat S for metabolism-related diseases.

BMS-212122 inhibits MTP, reduces lipids and plaque in animal tests.

gamma-Glu-Tyr (gamma-Glutamyltyrosine) is a kokumi peptide against dipeptidyl peptidase-IV (DPP-IV) and is used in the study of diabetes mellitus.

HIV-1 inhibitor-54: potent anti-HIV (EC50: 32 nM), targets WT HIV-1 IIIB in MT-4 cells for infection research.

Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor indicated for the study of allergic asthma, COPD and pulmonary fibrosis.

VBY-825 is a reversible inhibitor of cathepsin with high potency against cathepsins B, L, S and V.

PLGLAG is a peptide chain that acts as a linker in activatable cell-penetrating peptides (ACPPs). ACPPs containing the PLGLAG linker are primarily sensitive to MMP-2 and MMP-9 in vivo. PLGLAG is applicable in cancer research.

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor that inhibits Hep G2, MCF 7 and MCF 10A cells.

Napsagatran hydrate is a novel and specific inhibitor of thrombin.

Odiparcil is an orally active beta-d-thioxyloside analog.

ZINC09518833 is an α-ketoamide non-peptide proteasome inhibitor with an IC50 value of 12.4 μM. It can bind with both the active and inactive sites of the proteasome. ZINC09518833 shows promise for use in research related to multiple myeloma (MM).

MMP-13-IN-1, with an IC50 value of 16 nM, is a potent and selective inhibitor of MMP-13, suitable for atherosclerosis research [1].

Matriptase-IN-2 free base, a matriptase inhibitor with a K i of 5 nM, has potential applications in musculoskeletal system disorder research (WO2011023958A1; compound 432) [1].

HsClpP activator-1 (compound 24) is a potent activator of HsClpP, with an EC50 of 0.22 μM. It effectively inhibits cancer cell growth, exhibiting IC50 values ranging from 0.1 to 1 μM.

GB111-NH2, a cysteine cathepsin inhibitor, is applicable in cancer research [1].

Tyrosinase-IN-37 (Compound 3c) is a potent inhibitor of tyrosinase, with an IC50 value of 1.02 μM, which is 14 times more effective than kojic acid (IC50 of 14.74 μM). This compound effectively prevents the browning of Rosa roxburghii and can also inhibit browning not caused by tyrosinase.