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-P990395
    Anti-CXCR4/CD184 Antibody
    Anti-CXCR4/CD184 Antibody is a CHO-expressed human antibody that targets CXCR4/CD184. The Anti-CXCR4/CD184 Antibody has a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-CXCR4/CD184 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-CXCR4/CD184 Antibody
  • HY-115615
    VUF11207 TFA
    Agonist
    VUF11207 (Compound 29) TFA is a CXCR7 agonist (pKi of 8.1) that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
    VUF11207 TFA
  • HY-P4095
    NoxaBH3
    NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1. NoxaBH3 binds to the endogenous CXCR4 ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells.
    NoxaBH3
  • HY-P10427
    DV1
    Antagonist
    DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models.
    DV1
  • HY-153240
    ACT-672125
    Antagonist
    ACT-672125 is a potent CXCR3 antagonist with IC50 value of 239 nM in human blood. ACT-672125 has activity for hERG with IC50 value of 18μM. ACT-672125 can be used for the research of autoimmune diseases.
    ACT-672125
  • 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.
    TIQ-15
  • HY-RS03404
    Cxcr3 Mouse Pre-designed siRNA Set A
    Inhibitor

    Cxcr3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cxcr3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Cxcr3 Mouse Pre-designed siRNA Set A
    Cxcr3 Mouse Pre-designed siRNA Set A
  • HY-P990393
    Anti-CXCL9 Antibody
    Anti-CXCL9 Antibody is a humanized antibody expressed in CHO cells, targeting CXCL9. The Anti-CXCL9 Antibody contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-CXCL9 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-CXCL9 Antibody
  • HY-P0172
    ATI-2341
    Agonist
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
    ATI-2341
  • 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-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-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-P4846
    Ac-Pro-Gly-Pro-OH
    Agonist
    Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and can be used as CXCR2 agonist. Ac-Pro-Gly-Pro-OH elicits bactericidal activity and inhibits lung inflammation, reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH enhances the production of type 1 cytokines (IFN-γ and IL-12) but inhibits the production of proinflammatory cytokines. Ac-Pro-Gly-Pro-OH has the potential for the research of sepsis.
    Ac-Pro-Gly-Pro-OH
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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