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-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
  • HY-N11723
    Catenarin
    		Inhibitor
    Catenarin, an anthraquinone compound, inhibits CCR5- and CXCR4-mediated chemotaxis. Catenarin reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), and calcium mobilization. Catenarin shows anti-inflammatory effect and suppresses leukocyte migration in the diabetes. Catenarin exhibits significant inhibitory effects against Gram-positive bacteria. Catenarin prevents type 1 diabetes (T1D) in nonobese diabetic mice[1][2].
    Catenarin
  • 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
  • HY-P2642
    Peptide 78
    		98.13%
    Peptide 78, a chemotactic cytokine, a 78 amino acid protein member of the IL-8 or C-X-C chemokine supergene family. ENA-78 plays an important role in the elicitation of predominantly neutrophils (PMNs) into the joints of rheumatoid arthritis (RA).
    Peptide 78
  • 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.
    CXCR2 antagonist 4
  • HY-167945
    AMD-3329
    		Inhibitor
    AMD-3329 is a potent and selective anti-HIV-1 and HIV-2 agent, exhibiting activity by inhibiting virus replication through binding to the chemokine receptor CXCR4, which serves as a co-receptor for the entry of X4 viruses.
    AMD-3329
  • HY-131374
    TN14003
    		Inhibitor
    TN14003 is a CXCR4 inhibitor. TN14003 has antitumor activity.
    TN14003
  • 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.
    CXCR4 antagonist 6
  • HY-172154
    SSB-2548
    		Inhibitor
    SSB-2548 is a CXCR-4 inhibitor. SSB-2548 can inhibit the proliferation, migration and induce apoptosis of acute myeloid leukemia cells. SSB-2548 has good gastrointestinal absorption and can be used in the research of leukemia.
    SSB-2548
  • HY-132936
    CXCR4 antagonist 2
    		Antagonist
    CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
    CXCR4 antagonist 2
  • HY-162505
    SQA1
    		Inhibitor
    SQA1, a squaramide (SQA) derivative, is a CCR6 antagonist with a Kd of 250 nM. SQA1 is also a CXCR2 inhibitor. The intracellular pocket occupied by SQA1 overlaps with the G protein binding site and stabilizes the closed conformation of the intracellular pocket.
    SQA1
  • HY-P991567
    VX5
    		Modulator
    VX5 is a humanized IgG1κ monoclonal antibody inhibitor targeting BCA-1/CXCL13. VX5 significantly inhibits human CXCL13-mediated internalization of CXCR5, blocks both human and mouse CXCL13-dependent B-cells chemotaxis and migration (EC50s for 105 and 253 nM for human tonsillar and pre-B-697-hCXCR5 cells, respectively). VX5 can be used to study autoimmune diseases like multiple sclerosis and arthritis, and cancers like gastric lymphomas and colon cancer.
    VX5
  • HY-50912R
    Plerixafor octahydrochloride (Standard)
    		Antagonist
    Plerixafor (octahydrochloride) (Standard) is the analytical standard of Plerixafor (octahydrochloride). This product is intended for research and analytical applications. Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
    Plerixafor octahydrochloride (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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