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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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Caspase inhibitor
Z-WEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity. -
Caspase-3/7 Inhibitor
Caspase-3/7 Inhibitor I is a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM). -
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. -
Proteasome inhibitor
Dihydroeponemycin is an inhibitor of proteasome and antitumor reagent. -
Reversible thrombin inhibitor
Bivalirudin is a synthetic 20 residue peptide which reversibly inhibits thrombin. -
HIV-1 attachment inhibitor
BMS-663068 is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection.- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
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HIV-1 attachment inhibitor
BMS-663068 tris is an HIV-1 attachment inhibitor in development for the treatment of HIV-1 infection. -
CPG2 inhibitor
Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents. -
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. -
DPP-4 inhibitor
Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM. -
HIV protease inhibitor
Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates. -
Selective calpain inhibitor
Acetyl-Calpastatin (184-210) (human), selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 uM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio. -
Caspase-3 inhibitor
AZ 10417808, selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 uM). -
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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γ-secretase inhibitor
MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo. -
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
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DPP-4 inhibitor
PK 44 phosphate is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an IC50 value of 15.8 nM. -
Human cathepsin L inhibitor
SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G. -
MMP-13 inhibitor
WAY 170523 has been reported to be a selective and potent inhibitor of MMP-13. -
DPP-4 inhibitor
NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV with Ki and IC50 values of 11 nM and 14 nM, respectively. -
ADAM10 metalloprotease inhibitor
GI 254023X is a selective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17. -
Urokinase (uPA) inhibitor
4-Chlorophenylguanidine hydrochloride is a potent and specific inhibitor of uPA (urokinase). -
Urokinase (uPA) inhibitor
BC 11 hydrobromide, belective urokinase (uPA) inhibitor (IC50 = 8.2 μM). Inhibits clot lysis with no effect on clot formation and exhibits no activity at 8 other uPA related enzymes. -
MMP Inhibitor
Batimastat is an anticancer drug that belongs to the family of drugs called angiogenesis inhibitors. Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. -
serine/threonine phosphatase inhibitor
Fumonisin B1 is a fungal metabolite produced by Fusarium moniliforme, that has been shown to inhibit protein serine/threonine phosphatases (PP1, PP2A, PP2B, PP2C, and PP5/T/K/H), and is most effective with PP5.