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CXCR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S8947 SX-682 SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumour MDSC recruitment and enhances T cell activation and antitumour immunity.
Biomolecules, 2025, 15(5)645
Cell Metab, 2024, 36(5):984-999.e8
Nat Commun, 2023, 14(1):4677
S8505 LY2510924 LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with an IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with a 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
S8869 UNBS5162 UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7).
Cell Discov, 2023, 9(1):104
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).
E7614 NBI-74330 NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
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.
S3951 Tannic acid Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.
S9725 Balixafortide (POL6326)

An orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist, Balixafortide (POL6326) is a compound of interest in this context.
S8309 ATI-2341 ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilisation.
E5984New ML339 ML339 is a potent and selective antagonist of CXCR6. ML339 antagonises CXCL16-induced β-arrestin recruitment and cAMP signalling 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.