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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. -
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. -
Gamma-secretase inhibitor
FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.- Tan YJ, .et al. , Future Med Chem, 2018, Sep 1;10(17):2039-2057 PMID: 30066578
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Proteasome Inhibitor
Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.- Tarantelli C, .et al. , Clin Cancer Res, 2018, Jan 1;24(1):120-129 PMID: 29066507
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HCV NS5A inhibitor
MK 8742, also known as Elbasvir, is a HCV NS5A inhibitor, which is an all-oral, interferon-free regimen for the treatment of HCV infection. -
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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DPP-IV inhibitor
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM). -
DPP-4 inhibitor
Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. -
Caspase inhibitor
Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models. -
Cysteine Protease inhibitor
Leupeptin hemisulfate is a reversible inhibitor of trypsin-like and cysteine proteases such as calpain. -
HIV-1 attachment inhibitor
BMS-626529 is a potent HIV-1 attachment inhibitor. BMS-663068 is also the phosphonooxymethyl prodrug of BMS-626529 that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells. -
Proteasome inhibitor
ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. -
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. -
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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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.