2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
  4. CXCR
  5. CXCR Antagonist

CXCR Antagonist

CXCR Isoform Comparison

CXCR Antagonists (99):

Cat. No. Product Name Effect Purity
  • HY-115493
    TIQ-15
    		Antagonist
    TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM.
  • HY-167851
    CCX662
    		Antagonist
    CCX662 is CXCR7 antagonist. CCX662 inhibits the binding of 125I-CXCL12 to CXCR7, with an IC50 of 9 nM. CCX662 can be used in anti-cancer research.
  • HY-111224
    GSK812397
    		Antagonist
    GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.
  • HY-147978
    CXCR4 antagonist 8
    		Antagonist
    CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration.
  • HY-118037
    VUF10132
    		Antagonist
    VUF10132 is a non-peptide CXCR3 receptor antagonist with anti-inflammatory activity, inhibiting diseases such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has high affinity for the human CXCR3 receptor but slightly lower affinity for the murine CXCR3 receptor. Additionally, VUF10132 exhibits inverse agonist properties at the CXCR3 receptor.
  • HY-136437
    CXCR4 antagonist 1
    		Antagonist
    CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity.
  • HY-163480
    PF-06835375
    		Antagonist
    PF-06835375 is a humanized IgG1 antibody selective against CXCR5 expressed on B cells, Tfh cells, and circulating Tfh-like (cTfh) cells. PF-06835375 can be used for the study of systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001)[1].
  • HY-139874
    CXCR2 antagonist 3
    		Antagonist
    CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues.
  • HY-168971
    Paeoniflorin-6′-O-benzene sulfonate
    		Antagonist
    Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model.
  • HY-146413
    HF50731
    		Antagonist
    HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM.
  • HY-129094
    ICT5040
    		Antagonist
    ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells.
  • HY-P10429
    RCP168
    		Antagonist
    RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors.
  • HY-173052
    SLW131
    		Antagonist
    SLW131 (Compound 10) is the antagonist for CCR7 with a good affinity of Ki of 9.85 nM. SLW131 inhibits CCL19-induced Go protein activation with an IC50 of 29.4 μM, inhibits β-arrestin2 recruitment with an IC50 of 6.0 μM. SLW131 inhibits CCL19-induced cell morphological changes in primary BMDCs, and CCR7-mediated migration in mouse CD4+ T cell.
  • HY-144780
    CXCR2 antagonist 4
    		Antagonist
    CXCR2 antagonist 4 (compound 7) is a potent CXCR2 antagonist with an IC50 value of 0.13 μM. CXCR2 antagonist 4 can inhibit CXCL8-induced cytosolic calcium increase (IC50 = 27 μM). CXCR2 antagonist 4 can be used for researching anticancer.
  • HY-146401
    CXCR4 antagonist 6
    		Antagonist
    CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice.
  • HY-132936
    CXCR4 antagonist 2
    		Antagonist
    CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
  • HY-110099
    (±)-NBI-74330
    		Antagonist
    (±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model.
  • HY-123819
    KRH-1636
    		Antagonist
    KRH-1636 is a CXC chemokine receptor (CXCR) 4 antagonist. KRH-1636 can be used in HIV-1 research.
  • HY-10046R
    Plerixafor (Standard)
    		Antagonist
    Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. 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.