Proteases/Proteasome

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

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

Tyropeptin A-4 is used as a proteasome inhibitor.

AZD-7295 (A-689) is an NS5A inhibitor that may be used to treat HCV infection.

JW480 is a potent and selective inhibitor of KIAA1363, a serine hydrolase enzyme.

ND-378 is a potent and selective inhibitor of MMP-2 with no inhibition on MMP-9 and MMP-14.

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

ABP 25 is a highly potent and selective activity-based probe (ABP) for cathepsin K imaging.

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

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

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

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

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

Thrombin inhibitor 1 is a potent inhibitor of thrombin (Ki: 0.66 nM, 2xaPTT=0.43 μM).

LM-030, also known as BPR277, is a novel inhibitor of kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2).

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

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

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

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

Ro 32-7315 is a selective inhibitor of ADAM17.

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).

H-Gly-Pro-Hyp-OH, a peptide dipeptidyl peptidase 4 (DPP-4) inhibitor with an inhibition concentration (IC50) of 2.51 mM, effectively hinders the activity of the DPP-4 enzyme.

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.

Flovagatran sodium, a thrombin inhibitor, is used potentially for the treatment of thrombosis.

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

BAY-320 is a Bub1 inhibitor. With an IC50 of 680 nM for human Bub1 in the presence of 2 mM ATP.

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

AA74-1 is a potent, selective APEH inhibitor that significantly enhances T-cell proliferation by inhibiting APEH activity [1].

MDL 27324 is an inhibitor of human neutrophil elastase.

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

LMP7-IN-2 is an inhibitor of LMP7 and may be utilized in the treatment of associated inflammatory diseases and disorders [1].

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

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.

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

MDL 101146 is an orally active neutrophil elastase inhibitor.

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

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].

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

MMP-145 is used as a protease inhibitor.

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].

BMS-189664 is an inhibitor of thrombin.

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.

GSK-625433: Homochiral inhibitor blocks HCV genotypes 1a/1b polymerase.

SQ 32056 is a cathepsin E inhibitor.

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-5, also known as compound 5, acts as a proteasome inhibitor [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

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

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].

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

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

HCV-IN-44 (compound 28) is an inhibitor of the HCV NS5B protein, efficacious in suppressing HCV virus replication and useful for researching HCV infection [1].

Yimitasvir diphosphate, also known as Emitasvir, is an orally-administered inhibitor of the hepatitis C virus (HCV) nonstructural protein 5A (NS5A).

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

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

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.

MeOSuc-AAPV-CMK (Elastase Inhibitor III) serves as an inhibitor of elastase, as well as cathepsin G and proteinase 3, and impedes leukocyte elastase-mediated

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

Ecallantide (DX-88) is a recombinant inhibitor specifically targeting plasma kallikrein, which serves to impede the synthesis of bradykinin.

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).

BMS-189664 HCl is a selective and orally active thrombin active site inhibitor.

Z-DEVD-CMK irreversibly inhibits various cathepsins in vitro [1].

DCLK1-IN-2 (Compound I-5) is a potent inhibitor of DCLK1, exhibiting an IC50 of 171.3 nM, and demonstrates significant antiproliferative effects on SW1990 cell

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

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

I-XW-053 is an inhibitor of capsid targeted HIV-1 replication using the hybrid structure based method to block the interface between CA N-terminal domains (NTD-

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.

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

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

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

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

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

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.

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

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

Faldaprevir sodium: HCV treatment, inhibits NS3/NS4A protease, P-glycoprotein, CYP3A4, UGT1A1.

Pyridoxatin: fungal metabolite; blocks TBARS production, prevents AAPH-induced hemolysis, and acts against C. albicans.

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.

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].

NAPAP is a thrombin inhibitor with potent anticoagulant activity (Ki: 2.1 nM). It selectively inhibits thrombin through a rapid binding mechanism while exhibiting weaker inhibition of trypsin, Factor Xa, and plasmin. NAPAP can be utilized for research into thrombotic conditions, including venous thrombosis and myocardial infarction.