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angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
metalloendopeptidase inhibitor
Phosphoramidon Disodium Salt is a metalloendopeptidase inhibitor. -
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. -
protein phosphatase inhibitor
Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1. -
Caspase-9 Inhibitor
Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Wenquan Liang, .et al. , Sci Rep, 2016, 6: 38267 PMID: 27905569
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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. -
20S proteasome inhibitor
Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity. -
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. - Elastase Inhibitor is a potent, irreversible inhibitor of human neutrophil elastase (HNE).
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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. -
gamma-secretase modulator
gamma-secretase modulator 3 is a gamma-secretase modulator. -
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. -
Fluorogenic caspase substrate
Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC. -
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).