| S5079 |
Sitagliptin
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Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes.
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Small Sci, 2025, 5(12):e202500140
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Pharmacol Res, 2025, 215:107696
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Sci Rep, 2025, 15(1):30226
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| S3033 |
Vildagliptin
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Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.
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Int J Mol Sci, 2024, 25(18)9760
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J Clin Invest, 2023, 133(12)e165933
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Oncoimmunology, 2023, 12(1):2268257
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| S4002 |
Sitagliptin phosphate monohydrate
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Sitagliptin phosphate monohydrate (MK-0431) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.
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Small Sci, 2025, 5(12):e202500140
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J Cell Mol Med, 2025, 29(11):e70581
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Front Oncol, 2021, 11:704024
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| S8455 |
Talabostat (Val-boroPro, PT-100) Mesylate
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Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities.
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Int J Mol Sci, 2025, 26(5)2237
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J Oral Microbiol, 2024, 16(1):2373040
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Brain Res, 2024, S0006-8993(24)00383-4
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| S9631 |
Puromycin aminonucleoside
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Puromycin aminonucleoside (NSC 3056, PAN, Stylomycin aminonucleoside, ARDMA, SAN), the aminonucleoside portion of the antibiotic puromycin, is a reversible inhibitor of dipeptidyl-peptidase II and cytosol alanyl aminopeptidase that induces apoptosis in mesangial cells (MCs) accompanied by declined cell viability and enhanced inflammatory response.This compound can be used to induce animal models of Kidney Disease.
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PLoS Pathog, 2025, 21(9):e1013549
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bioRxiv, 2025, 2025.08.15.670603
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mBio, 2024, 15(12):e0194524
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| S1540 |
Saxagliptin (BMS-477118)
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Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with an IC50 of 26 nM.
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Turk J Pharm Sci, 2019, 16(2):227-233
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Cancer Cell, 2018, 34(4):659-673
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J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257
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| S8565 |
MK-3102 (Omarigliptin)
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Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
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NYMC Student Theses and Dissertations, 2023,
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Acta Pharmacol Sin, 2021, 1-9
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Front Behav Neurosci, 2021, 15:705579
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| S2868 |
Alogliptin (SYR-322) benzoate
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Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.
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Cell Rep, 2017, 20(7):1692-1704
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| S5365 |
Alogliptin
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Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.
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Sci Adv, 2021, 7(27)eabh3032
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| E1188 |
Brensocatib
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Brensocatib (AZD7986, INS1007) is an oral, selective, reversible inhibitor of dipeptidyl peptidase-1 (DPP-1). It reduces the activity of all major neutrophil serine proteases (NSPs) including, neutrophil elastase (NE), proteinase 3 (PR3), and cathepsin G (CatG) in patients with bronchiectasis.
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Nat Commun, 2024, 15(1):6519
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