| S6645 |
AZD5069
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AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.
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The Journal of Clinical Investigation, 2025, e183541
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Biomed Pharmacother, 2025, 188:118203
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Biomedicine & Pharmacotherapy, 2025, 118203
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| S8030 |
AMD3100 (Plerixafor)
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Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.
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Theranostics, 2025, 15(18):9819-9837
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Cell Mol Life Sci, 2025, 82(1):280
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iScience, 2025, 28(1):111564
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| S7651 |
SB 225002
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SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
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Adv Sci (Weinh), 2025, 12(8):e2411711
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Theranostics, 2025, 15(7):2852-2869
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Cancer Immunol Res, 2025, 10.1158/2326-6066.CIR-24-1194
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| S3013 |
Plerixafor (AMD3100) 8HCl
|
Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 8HCl is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor can be used as an anti-HIV agent.
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Angiogenesis, 2025, 28(3):26
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bioRxiv, 2025, 2025.08.29.673113
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bioRxiv, 2025, 2025.05.28.656643
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| S8640 |
Reparixin (Repertaxin)
|
Reparixin (Repertaxin, DF 1681Y) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. It inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. This compound also inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).
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Immunity, 2025, S1074-7613(25)00139-6
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Nat Commun, 2025, 16(1):4128
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Nat Commun, 2025, 16(1):7156
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| S2912 |
WZ811
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WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.
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Front Immunol, 2024, 15:1389411
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Neural Regen Res, 2024, 10.4103/NRR.NRR-D-24-00081
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Cells, 2024, 13(5)408
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| S8506 |
Navarixin (SCH-527123)
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Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.
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J Immunother Cancer, 2025, 13(12)e012606
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Biomolecules, 2025, 15(5)645
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iScience, 2024, 27(8):110562
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| S8947 |
SX-682
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SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity.
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Nature Communications, 2025, 17(1)
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Biomolecules, 2025, 645
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Biomolecules, 2025, 15(5)645
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| S8813 |
LIT-927
|
LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma.
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Cell Mol Life Sci, 2025, 82(1):280
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Nat Commun, 2024, 15(1):10413
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Nat Commun, 2023, 14(1):5534
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| S4785 |
Nicotinamide N-oxide
|
Nicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. This compound is novel, potent, and selective antagonists of the CXCR2 receptor.
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Front Immunol, 2025, 16:1552993
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Inflammation, 2024,
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Cell Rep, 2023, 42(6):112566
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