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CXCR Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Theranostics, 2025, 15(18):9819-9837
Cell Mol Life Sci, 2025, 82(1):280
iScience, 2025, 28(1):111564
Verified customer review of AMD3100 (Plerixafor)
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
Verified customer review of SB 225002
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.
Angiogenesis, 2025, 28(3):26
bioRxiv, 2025, 2025.08.29.673113
bioRxiv, 2025, 2025.05.28.656643
Verified customer review of Plerixafor (AMD3100) 8HCl
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
Verified customer review of WZ811
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
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
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
S9516 SB 265610 SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site.
PLoS One, December 09, 2016, e0167169
Biomed Pharmacother, 2025, 188:118203
Biochem Biophys Res Commun, 2025, 785:152706
S8505 LY2510924 LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L.
Front Physiol, 2024, 15:1349119
Frontiers in Physiology, 2024, 1349119
Nat Commun, 2023, 14(1):2207
S6620 Danirixin (GSK1325756) GSK1325756 (Danirixin) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.
Redox Biology, August 20, 2024, 103323
Redox Biol, 2024, 76:103323
Redox Biology, 2024, 103323
S2879 AMD3465 hexahydrobromide AMD3465 is a monomacrocyclic CXCR4 antagonist.
Front Oncol, 2021, 11:708915
S9665 Motixafortide (BL-8040, BKT140) Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
King's College London, 2023,
S6617 MSX-122 MSX-122 (Q-122) is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
Cellular and Molecular Gastroenterology and Hepatology, 2024, 17(3):321-346
Cellular and Molecular Gastroenterology and Hepatology, 2024, 321-346
Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.007
S9725 Balixafortide (POL6326)

An orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist, Balixafortide (POL6326) is a compound of interest in this context.
Kaohsiung Journal of Medical Sciences, 2022, 781-789
E1318 Mavorixafor Mavorixafor (AMD-070) is a potent, selective CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding.
S0292 MSX-127 MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist.
S0293 MSX-130 MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4).
E4650 Ladarixin Ladarixin(DF 2156A free base) is a small molecule, orally available, allosteric and non-competitive antagonist of dual CXCR1 and CXCR2. It is able to reduce the acute and chronic neutrophilic influx, and can be used in research of Asthma, Idiopathic Pulmonary Fibrosis, Influenza-A infection and COPD, cutaneous and uveal melanoma conditions.
E5984New ML339 ML339 is a potent and selective antagonist of CXCR6. ML339 antagonizes CXCL16-induced β-arrestin recruitment and cAMP signaling through the human CXCR6 receptor with IC50 values of 0.3 and 1.4 μM, respectively. ML339 shows no inhibitory activity against CXCR5, CXCR4, and CCR6. ML339 can be used as a potential agent for prostate cancer research.
S0438 TAK-779 TAK-779(Takeda 779), a nonpeptide compound,  is a potent antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5. It also exhibits highly potent and selective inhibition of R5 HIV-1 replication with EC50 and EC90 of 1.2 and 5.7 nM, respectively. It also suppresses the development of the cytokine storm in the murine model of the SARS-CoV-2-related acute respiratory distress syndrome.