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

CXCR

CXC chemokine receptors; C-X-C motif chemokine receptors

CXCR

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CXCRs (CXC chemokine receptors) are integral membrane proteins that specifically bind and respond to cytokines of the CXC chemokine family. They represent one subfamily of chemokine receptors, a large family of G protein-linked receptors that are known as seven transmembrane (7-TM) proteins, since they span thecell membrane seven times. There are currently seven known CXC chemokine receptors in mammals, named CXCR1 through CXCR7. CXCR1 and CXCR2 are closely related receptors that recognize CXC chemokines that possess an E-L-R amino acid motif immediately adjacent to their CXC motif. CXCR3 is expressed predominantly on T lymphocytes. CXCR4 is the receptor for a chemokine known as CXCL12 (or SDF-1) and, as with CCR5, is utilized by HIV-1 to gain entry into target cells. The chemokine receptor CXCR5 is selectively expressed on B cells and is involved in lymphocyte homing and the development of normal lymphoid tissue. CXCR6 was formerly called three different names (STRL33, BONZO, and TYMSTR) before being assigned CXCR6 based on its chromosomal location and its similarity to other chemokine receptors in its gene sequence. CXCR7 was originally called RDC-1 (an orphan receptor) but has since been shown to cause chemotaxis in T lymphocytes in response to CXCL12 (the ligand for CXCR4) prompting the renaming of this molecule as CXCR7.

CXCR Isoform Specific Products:

CXCR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P10444
    DOTA Conjugated JM#21 derivative 7
    DOTA Conjugated JM#21 derivative 7 (compound Ligand-7) is a derivative of CXCR4 targeting peptide conjugated with DOTA and can be used to produce radioligands. Radiolabeled DOTA Conjugated JM#21 derivative 7, i.e., 177Lu-DOTA, has excellent CXCR4 tumor targeting. In vitro biodistribution results of 177Lu-DOTA showed very low uptake in all non-targeted organs except kidney. DOTA Conjugated JM#21 derivative 7 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA Conjugated JM#21 derivative 7
  • HY-P1949
    Cyclic MKEY
    Cyclic MKEY is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY also protects against stroke-induced brain injury in mice.
    Cyclic MKEY
  • HY-P990392
    Anti-CXCL8/IL-8 Antibody
    Anti-CXCL8/IL-8 Antibody is a human antibody expressed in CHO cells that targets CXCL8/IL-8. The Anti-CXCL8/IL-8 Antibody is composed of a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-CXCL8/IL-8 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-CXCL8/IL-8 Antibody
  • HY-RS03405
    Cxcr3 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cxcr3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr3 Rat Pre-designed siRNA Set A
    Cxcr3 Rat Pre-designed siRNA Set A
  • 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.
    Paeoniflorin-6′-O-benzene sulfonate
  • HY-W019787
    BAM-12P
    		Activator
    BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM.
    BAM-12P
  • HY-N0011R
    Baohuoside I (Standard)
    		Inhibitor
    Baohuoside I (Standard) is the analytical standard of Baohuoside I. This product is intended for research and analytical applications. Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
    Baohuoside I (Standard)
  • HY-RS03412
    Cxcr6 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cxcr6 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr6 Rat Pre-designed siRNA Set A
    Cxcr6 Rat Pre-designed siRNA Set A
  • 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.
    HF50731
  • HY-P10301
    CXCL9(74-103)
    CXCL9(74-103) is a derivative peptide of CXCL9 that has a high affinity for glycosaminoglycans (GAGs) and can bind to GAGs. CXCL9(74-103) possesses anti-angiogenic properties, capable of reducing EGF, VEGF165, and FGF-2-mediated angiogenesis processes in vitro, without exhibiting cytotoxicity.
    CXCL9(74-103)
  • HY-P10333
    LIH383
    		Agonist
    LIH383 is an agonist of ACKR3 (CXCR7) (EC50=0.61 nM). LIH383 efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.
    LIH383
  • HY-P4109
    vMIP-II (1-21)
    		Inhibitor
    vMIP-II (1-21) (NT21MP) is an inhibitor of CXCR4. vMIP-II (1-21) interacts broadly with CC and CXC chemokine receptors. vMIP-II (1-21) inhibits CXCR4 by competing with 125I-SDF-1R for binding sites (IC50=190 nM).
    vMIP-II (1-21)
  • HY-P10321
    HBP08
    HBP08 is a selective inhibitor of CXCL12/HMGB1 interaction. HBP08 has a high affinity for HMGB1 (Kd=0.8 μM). HBP08 inhibits CXCL12-mediated cell migration.
    HBP08
  • HY-D2310
    CXCR2 Probe 1
    CXCR2 Probe 1 (Compound [18F]16b) is a selective ligand for CXCR2 and is a radiotracer for PET imaging of neutrophils in inflammatory diseases.
    CXCR2 Probe 1
  • HY-15319A
    (±)-AMG 487
    		Inhibitor
    (±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
    (±)-AMG 487
  • 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.
    ICT5040
  • 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.
    RCP168
  • HY-RS03411
    Cxcr6 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Cxcr6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cxcr6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr6 Mouse Pre-designed siRNA Set A
    Cxcr6 Mouse Pre-designed siRNA Set A
  • 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.
    SLW131
  • HY-119234
    CX4338
    CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis.
    CX4338
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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