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>

<p>PNU-103017 is an inhibitor of HIV protease.</p>

<p>L-689502 is a potent HIV-l protease inhibitor (IC50: 1 nM).</p>

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

<p>Petesicatib is an inhibitor of cathepsin S. Petesicatib used in the research of immune diseases.</p>

<p>SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).</p>

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

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

<p>PDDC inhibitor (Phenyl (R)-(1-(3-(3,4-dimethoxyphenyl)-2,6-dimethylimidazo[1,2-b]pyridazin-8-yl)pyrrolidin-3-yl)carbamate) is an nSMase2 inhibitor.</p>

<p>Filibuvir (PF-00868554) inhibits HCV polymerase genotypes 1a/1b, EC50s 59 nM.</p>

<p>Ac-YVAD-AOM is a selective and potent caspase-1 inhibitor showing antitumor activity and potential analgesic activity.</p>

<p>Collagen proline hydroxylase inhibitor-1 具有抗纤维增生活性。</p>

<p>ZED-1227 (TAK-227) is a TG2 inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Diseas</p>

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

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

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

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

<p>BMS-212122 inhibits MTP, reduces lipids and plaque in animal tests.</p>

<p>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.</p>

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

<p>HCVNS5B polymerase-IN-2 (Compound 298) is an inhibitor of the Ns5b polymerase. It holds potential for research into the treatment of hepatitis C virus (HCV) infections.</p>

<p>(2R,3S)-Emricasan ((2R,3S)-PF 03491390) is an isomer of Emricasan. This compound acts as an orally effective irreversible pan-caspase inhibitor. (2R,3S)-Emricasan inhibits the increase in caspase-3 activity induced by Zika virus (ZIKV) and protects human cortical neural progenitor cells.</p>

<p>Beclabuvir blocks HCV NS5B polymerase at thumb site 1, effective on genotypes 1, 3, 4, 5 with IC50 &lt;28 nM.</p>

<p>Immunoproteasome Activator 1 (compound A) is a selective immunoproteasome activator that enhances the presentation of individual MHC-I binding peptides by over 100 times. It binds to the proteasomal structural subunit PSMA1 and facilitates the association of the proteasome activators PA28α/β (PSME1/PSME2) with the immunoproteasome.</p>

<p>UK-370106 is a potent and highly selective inhibitor of MMP-3 with IC50 of 23 nM and MMP-12 with IC50 of 42 nM, and potently inhibits cleavage of [3H]-</p>

<p>Isobutylamido thiazolyl resorcinol is a tyrosinase (Tyrosinase) inhibitor that prevents pigment deposition induced by ultraviolet radiation.</p>

<p>LK-732 is a thrombin inhibitor with antithrombotic activity. It exhibits dose-dependent inhibition in models of hypercoagulability, with an IC50 value of 1.3 mg/kg. LK-732 is used in cardiovascular and cerebrovascular research.</p>

<p>Boc 3 Arg is a tert-butyl carbamate-protected arginine compound. It serves as an efficient tag that induces degradation by directly targeting proteins to the 20S proteasome.</p>

<p>3-Aminobenzene-1,2-diol (compound C8) is an inhibitor of matrix metalloproteinases (MMP), with IC50 values of 20, 26, 16, and 16.3 μM against MMP-2, MMP-8, MMP-9, and MMP-14, respectively.</p>

<p>TGase2-IN-1 (Compound 22) is an orally effective TGase2 inhibitor with an IC50 of 1.12 µM. It inhibits TGase2 in human retinal microvascular endothelial cells with a strikingly lower IC50 of 0.07 µM. The oral bioavailability of TGase2-IN-1 is 74.6%. Additionally, it can suppress retinal vascular leakage in a mouse model of diabetes induced by Streptozotocin.</p>

<p>Tyrosinase-IN-39 (compound 5r) is a competitive inhibitor of tyrosinase, with an IC50 of 6.4 μM, and is used in the study of skin diseases.</p>