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cathepsin C substrate
Gly-Phe-beta-naphthylamide is a cathepsin C substrate. The compound is described to accumulate inside lysosomes leading to their destruction. -
gamma-secretase inhibitor
Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). -
neprilysin inhibitor
AHU-377 is an inhibitor of neprilysin with IC50 value of 5nM. - 25-hydroxy Cholesterol is a side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of sterol regulatory element binding proteins (SREBPs) to suppress endogenous cholesterol synthesis in various cell types
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DPIV and DP8/9 inhibitor
DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively. -
Neutrophil elastase inhibitor
Sivelestat sodium salt is a selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. It inhibits NF-kB activation and LTB4-induced neutrophil transmigration in vitro.- Shasha He, .et al. , Nature Biomedical Engineering, 2023, 7: 281-297
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Cysteine Protease inhibitor
Leupeptin hemisulfate is a reversible inhibitor of trypsin-like and cysteine proteases such as calpain. -
Neutrophil elastase inhibitor
Sivelestat is a cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase). -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
HIV protease inhibitor
Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM. -
aspartic protease inhibitor
Pepstatin A is a potent aspartic protease inhibitor, and also inhibits HIV replication. -
serine protease inhibitor
Aprotinin is a small protein serine protease inhibitor, used to reduce perioperative blood loss and transfusion.- Xi Yu, .et al. , Neuroreport, 2022, Nov 2;33(16):705-713 PMID: 36165031
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phosphatase inhibitor
(-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor. -
DPP-4 inhibitor
Trelagliptin is a highly selective, long-acting DPP-4 inhibitor. -
DDP-4 inhibitor
Sitagliptin is an oral antihyperglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class.- Hae Jin Kim, .et al. , Korean J Physiol Pharmacol, 2018, Nov; 22(6): 713-719 PMID: 30402032
- Chintan N. Koyani, .et al. , Front Physiol, 2018, 9: 1622 PMID: 30487758
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Glutaminase inhibitor
CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.
- Beatriz Giesen, .et al. , Pharmaceutics, 2021, Feb 23;13(2):295 PMID: 33672398
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osteoblast differentiation inducer
Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP?\2/p38 and ERK1/2 pathway. Asperosaponin ?? inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB. -
Calpain Inhibitor
Calpain Inhibitor II, ALLM is a cell-permeable inhibitor of calpain I, calpain II, cathepsin L and cathepsin B with Ki values of 120 nM, 230 nM, 0.6 nM and 100 nM, respectively. -
HLE inhibitor
Elastase Inhibitor, SPCK is a potent, irreversible inhibitor of human leukocyte elastase (HLE) (Ki = 10 uM). -
Caspase inhibitor
Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM).- Anna L Koessinger, .et al. , Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. , Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Davide Pradella, .et al. , Nat Commun, 2021, 12: 4872 PMID: 34381052
- Haschka MD, .et al. , Cell Death Differ, 2020, Feb 3 PMID: 32015503
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20S proteasome inhibitor
AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. -
direct thrombin inhibitor
Dabigatran etexilate mesylate is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM. -
thrombin inhibitor
Dabigatran ethyl ester, which is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity. -
HIV protease inhibitor
Fosamprenavir Calcium Salt is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug. -
HCV Protease inhibitor
MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development. -
HCV Protease inhibitor
MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development. -
HCV Protease inhibitor
MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development. -
Fluorogenic caspase substrate
Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC. -
Gamma-secretase modulator
Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25. -
DPP-4 inhibitor
DPPI 1c hydrochloride is a dicyanopyrrolidine compound that acts as a slow-binding and active site-targeting inhibitor of CD26 (DPP 4), with an IC50 = 106 nM and little activity against DPP II, DPP III, DPP VIII, DPP IX, FAP, or APP even at concentrations as high as 30 μM. -
Aminopeptidase inhibitor
Fumagillin is a complex natural product antibiotic which covalently binds a key histidine residue of methionine aminopeptidase type II (MetAP-2), inhibiting endothelial cell proliferation and angiogenesis. -
Caspase-3 inhibitor
Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM).- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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Calpain Inhibitor III
MDL 28170 is a cell permeable selective inhibitor of Calpain 1, a Ca2+-dependent cysteine protease which has been implicated in apoptosis of immune cells as well as neuronal cells.- Barker BS, .et al. , Neuroscience, 2019, Nov 26. pii: S0306-4522(19)30796-1 PMID: 31783100
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Non-peptide calpain inhibitor
PD 150606 is a cell-permeable, non-competitive, selective, non-peptide Ca2+ dependent calpain inhibitor for calpain-1 and for calpain-2 directed towards the Ca2+ binding sites of calpain.- Hisamatsu Y, .et al. , Bioconjug Chem, 2017, Feb 15;28(2):507-523 PMID: 28032992