| S7540 |
SB273005
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SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
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EMBO J, 2025, 10.1038/s44318-025-00565-3
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bioRxiv, 2025, 2025.04.25.650475
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Cancer Lett, 2024, 582:216597
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| S7077 |
Cilengitide trifluoroacetate
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Cilengitide (EMD 121974, NSC 707544) is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.
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J Neuroinflammation, 2025, 22(1):168
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Int J Mol Sci, 2025, 26(6)2465
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Microbiol Spectr, 2025, 13(2):e0222124
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| S6387 |
Cilengitide (EMD 121974)
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Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-707544) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5 with IC50 of 4 and 79 nM, respectively.
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Nat Commun, 2025, 16(1):2254
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NPJ Regen Med, 2024, 9(1):4
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World J Gastroenterol, 2024, 30(7):728-741
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| S8008 |
RGD peptide (Arg-Gly-Asp)
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RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins.
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Adv Sci (Weinh), 2025, 12(18):e2417447
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J Sport Health Sci, 2024, S2095-2546(24)00124-8
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iScience, 2024, 27(3):109119
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| S8454 |
ATN-161
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ATN-161 is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
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Nat Commun, 2025, 16(1):6531
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Nat Commun, 2025, 16(1):9183
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Regen Biomater, 2025, 12:rbaf099
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| S7834 |
Cyclo(-RGDfK) TFA
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Cyclo(-RGDfK) TFA is the salt product of Cyclo(-RGDfK) and trifluoroacetic acid (TFA). The addition of TFA enhances stability and biocompatibility. This compound effectively targets tumor microvessels and cancer cells by specifically binding to the cell surface Integrin αvβ3.
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Pharmaceuticals (Basel), 2025, 18(4)549
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In Vitro Cell Dev Biol Anim, 2025, 10.1007/s11626-025-01101-7
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Sci Adv, 2024, 10(43):eadp4726
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| S7844 |
Cyclo(RGDyK) TFA
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Cyclo(RGDyK) TFA is a salt formed by the combination of Cyclo(RGDyK) and trifluoroacetate (TFA). It is an effective and selective Integrin αvβ3 inhibitor with a low IC50 value (e.g., 20 nM). This compound is of great significance in the treatment of cardiovascular diseases, osteoporosis, inflammation and tumors.
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J Clin Invest, 2024, e175147
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JBMR Plus, 2024, 8(7):ziae066
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Cell Commun Signal, 2023, 10.1186/s12964-022-01027-7
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| S8306 |
Leukadherin-1
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Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1 (an agonist for the complement receptor 3 (CD11b/CD18)).
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International Immunopharmacology, 2023, Volume 118
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Int Immunopharmacol, 2023, 118:110024
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Front Immunol, 2022, 13:919444
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| S2885 |
A-205804
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A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.
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Cell Biol Toxicol, 2024, 40(1):90
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Stem Cell Res Ther, 2022, 13(1):218
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Am J Rhinol Allergy, 2022, 19458924221086061
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| S3714 |
Lifitegrast
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Lifitegrast (SAR1118,SHP-606) is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.
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Med Oncol, 2024, 41(8):188
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World J Gastroenterol, 2023, 29(20):3103-3118
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Med Chem Res, 2022, 31(4):555-579
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