Proteases/Proteasome

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

<p>Tyropeptin A-4 is used as a proteasome inhibitor.</p>

<p>BMS-189664 is an inhibitor of thrombin.</p>

<p>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].</p>

<p>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].</p>

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

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

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

<p>Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: &lt;20 nM).</p>

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

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

<p>HIV-1 protease-IN-11 (compound 34a), an HIV-1 protease inhibitor, demonstrates potent inhibition with an IC50 of 0.41 nM and maintains substantial efficacy</p>

<p>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.</p>

<p>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</p>

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

<p>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].</p>

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

<p>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).</p>

<p>M109S is a novel small molecule that shields cells from mitochondria-dependent apoptosis, demonstrating effectiveness both in vitro and in vivo.</p>

<p>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.</p>