CXCR Antagonists

Cat.No.	Product Name	Information	Product Use Citations
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
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.	Angiogenesis, 2025, 28(3):26 bioRxiv, 2025, 2025.08.29.673113 bioRxiv, 2025, 2025.05.28.656643
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.	J Immunother Cancer, 2025, 13(12)e012606 Biomolecules, 2025, 15(5)645 iScience, 2024, 27(8):110562
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.	Cell Mol Life Sci, 2025, 82(1):280 Nat Commun, 2024, 15(1):10413 Nat Commun, 2023, 14(1):5534
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
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.	Biomed Pharmacother, 2025, 188:118203 Biomolecules, 2025, 15(5)645 Cell Rep, 2022, 38(10):110490
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 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 Biol, 2024, 76:103323 Theranostics, 2019, 9(18):5332-5346
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.	Biomed Pharmacother, 2025, 188:118203 Biochem Biophys Res Commun, 2025, 785:152706
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).	Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.007
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.
S9725	Balixafortide (POL6326)	An orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist, Balixafortide (POL6326) is a compound of interest in this context.
E5984^New	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.