1. Signaling Pathways
  2. GPCR/G Protein
  3. CXCR
  4. CXCR Antagonist

CXCR Antagonist

CXCR Antagonists (74):

Cat. No. Product Name Effect Purity
  • HY-10046
    Antagonist ≥98.0%
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
  • HY-16711
    Antagonist 99.87%
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
  • HY-10198
    Antagonist 99.13%
    Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
  • HY-119259
    AZD8309 is an orally active antagonist of CXCR2. AZD8309 has the ability to regulate the transmigration of neutrophils. AZD8309 can be used in the study of inflammatory diseases.
  • HY-P99272
    Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models.
  • HY-50912
    Plerixafor octahydrochloride
    Antagonist ≥98.0%
    Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
  • HY-19855
    Antagonist 99.63%
    AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
  • HY-10017
    SCH 546738
    Antagonist 98.71%
    SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
  • HY-P0171
    Antagonist 99.03%
    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
  • HY-15320
    Antagonist 99.62%
    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.
  • HY-50101A
    Mavorixafor trihydrochloride
    Antagonist 98.69%
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-13406
    Antagonist 99.73%
    TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
  • HY-101458A
    IT1t dihydrochloride
    Antagonist 99.89%
    IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-19519
    Antagonist 98.05%
    Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma.
  • HY-P1682A
    Balixafortide TFA
    Antagonist 99.78%
    Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-122197
    Antagonist 99.88%
    ML339 is a potent and selective CXCR6 (IC50 of 140 nM) antagonist that is selective (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ). ML339 holds potential to advance the field of prostate cancer research.
  • HY-19867A
    Burixafor hydrobromide
    Antagonist ≥98.0%
    Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well anti-angiogenic drug that is of potential value in treating choroid neovascularization. Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction.
  • HY-139643
    CXCR7 antagonist-1
    Antagonist 99.97%
    CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).
  • HY-15478
    Antagonist ≥98.0%
    WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
  • HY-50688
    Antagonist ≥99.0%
    SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively.