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

CXCR

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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    CCX662
  • HY-119208
    VUF11211
    Inhibitor
    VUF11211 is an allosteric inverse CXCR3 agonist with a Kd of 0.65 nM.
    VUF11211
  • 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.
    GSK812397
  • HY-165428
    SCH-900875
    Inhibitor
    SCH-900875 is an orally active, brain-penetrant and selective CXCR3 receptor inhibitor, which also shows high selectivity over CXCR1 and CXCR2 receptors. SCH-900875 binds to CXCR3, blocking the binding of ligands CXCL9, CXCL10, and CXCL11, inhibiting downstream G protein and β-arrestin signaling pathways to suppress inflammatory cell migration. SCH-900875 is promising for research of autoimmune diseases (rheumatoid arthritis, multiple sclerosis) and inflammatory disorders (psoriasis, inflammatory bowel disease).
    SCH-900875
  • HY-151559
    Zn-DPA-maytansinoid conjugate 1
    Modulator
    Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
    Zn-DPA-maytansinoid conjugate 1
  • HY-146054
    CXCR4 modulator-2
    Modulator
    CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model.
    CXCR4 modulator-2
  • 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.
    CXCR4 antagonist 8
  • HY-N2573
    Corydalmine
    Inhibitor
    Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.
    Corydalmine
  • HY-W701397
    Nicotinamide N-oxide-d4
    Nicotinamide N-oxide-d4 is the deuterium labeled Nicotinamide N-oxide (HY-101407). Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
    Nicotinamide N-oxide-d<sub>4</sub>
  • 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.
    VUF10132
  • HY-136437
    CXCR4 antagonist 1
    Antagonist
    CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity.
    CXCR4 antagonist 1
  • HY-117823
    VUF11418
    Agonist
    VUF11418 is a CXCR3 activator. VUF11418 can be used in inflammation research.
    VUF11418
  • HY-125567
    Antileukinate
    Inhibitor
    Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
    Antileukinate
  • HY-161414
    trans-VUF25471
    Agonist
    trans-VUF25471 (Compound trans-3e) is a photoswitchable ACKR3 agonist. trans-VUF25471 binds and activates ACKR3 at 10-fold lower concentrations compared to its cis-isomer.
    trans-VUF25471
  • 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].
    PF-06835375
  • HY-173290
    PDE4D inhibitor 1
    Inhibitor
    PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.
    PDE4D inhibitor 1
  • HY-RS03410
    CXCR6 Human Pre-designed siRNA Set A
    Inhibitor

    CXCR6 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CXCR6 Human Pre-designed siRNA Set A
    CXCR6 Human Pre-designed siRNA Set A
  • HY-RS03402
    Cxcr2 Rat Pre-designed siRNA Set A
    Inhibitor

    Cxcr2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Cxcr2 Rat Pre-designed siRNA Set A
    Cxcr2 Rat Pre-designed siRNA Set A
  • HY-W104862
    4-Amino-D-phenylalanine
    Inhibitor 99.74%
    4-Amino-D-phenylalanine ([D-Phe(4-NH2)), a cyclic pentapeptide, inhibits CXCL12 binding to CXCR4 in FC131, with an IC50 of 0.1 μM.
    4-Amino-D-phenylalanine
  • 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.
    CXCR2 antagonist 3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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