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CXCR Antagonist/Inhibitors

Other Immunology & Inflammation Related Inhibitors

AhR STING COX IL Receptor gp120/CD4 NOD NADPH-oxidase ROS Nrf2 NOS

Isoform-selective Products

CXCR1 CXCR2 CXCR4 CXCR3

Cat.No.	Product Name	Information	Product Use Citations	Product Validations
S6645	AZD5069	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.	Clinical Cancer Research, June 03, 2024, 2497-2513 International Endodontic Journal, January 27, 2026, Online ahead of print The Journal of Clinical Investigation, 2025, e183541
S8030	AMD3100 (Plerixafor)	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.	Frontiers in Cell and Developmental Biology, September 13 2021, 662868 Cell Communication and Signaling, May 18 2018, 21 PLoS One, August 09 2017, e0182697
S7651	SB 225002	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.	Adv Sci (Weinh), 2025, 12(8):e2411711 Theranostics, 2025, 15(7):2852-2869 Cancer Immunol Res, 2025, 10.1158/2326-6066.CIR-24-1194
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.	International Journal of Molecular Medicine, November 22, 2017, 969-976 PLOS Pathogens, March 10, 2026, e1014040 Angiogenesis, 2025, 28(3):26
S8640	Reparixin (Repertaxin)	Reparixin (Repertaxin, DF 1681Y) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).	Acta Pharmaceutica Sinica B, September 2021, 2835-2849 bioRxiv, September 18, 2024, nan PLoS Pathogens, January 2, 2024, e1011902
S2912	WZ811	WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.	Front Immunol, 2024, 15:1389411 Neural Regen Res, 2024, 10.4103/NRR.NRR-D-24-00081 Cells, 2024, 13(5)408
S8506	Navarixin (SCH-527123)	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.	Cell Discovery, October 17, 2023, 104 International Journal of Molecular Sciences, August 17, 2022, 9275 J Immunother Cancer, 2025, 13(12)e012606
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.	Journal of Gastroenterology, November 03, 2022, 25-43 Autoimmunity, February 25, 2024, 2319207 bioRxiv, August 18, 2025, 2025.08.13.670216
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.	Front Immunol, 2025, 16:1552993 Inflammation, 2024, Cell Rep, 2023, 42(6):112566
S8682	AMG 487	AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.	Nat Commun, 2025, 16(1):3905 Sci Rep, 2025, 15(1):34262 Sci Rep, 2025, 15(1):20778
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