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-167851
    CCX662
    		Inhibitor 98.62%
    CCX662 is a selective CXCR7 inhibitor with human IC50 values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC50 of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4+/CXCR7+ cells. CCX662 can be used for the research of glioblastoma multiforme.
    CCX662
  • HY-P990638
    NI-0701
    		99.74%
    NI-0701 is a humanized antibody expressed in CHO cells that targets CCL5/RANTES. NI-0701 has a huIgG2 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for NI-0701 can be referenced as Human IgG2 lambda, Isotype Control (HY-P991206).
    NI-0701
  • HY-161735
    CXCR4-IN-3
    		Inhibitor 99.69%
    CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research.
    CXCR4-IN-3
  • HY-122058A
    KRH-3955 hydrochloride
    		Antagonist
    KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
    KRH-3955 hydrochloride
  • HY-P0172
    ATI-2341
    		Agonist 99.64%
    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-110269
    VUF 11222
    		Agonist 99.91%
    VUF 11222 (Compound 38) is a CXCR3 non-peptide-like agonist. VUF 11222 can be used in the study of inflammation.
    VUF 11222
  • HY-114244
    USL311
    		Antagonist 99.97%
    USL311 is an orally active CXCR4 inhibitor. USL311 blocks the activity of the CXCR4 receptor. USL311 is applicable to research related to various cancers including breast cancer, bladder cancer, colon cancer, rectal cancer, liver cancer and glioblastoma.
    USL311
  • HY-P10552
    pCXCL8-1aa
    		Inhibitor 98.13%
    pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis.
    pCXCL8-1aa
  • HY-P990639
    NI-0801
    NI-0801 is a humanized antibody expressed in CHO, targeting CXCL10/IP-10. NI-0801 contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for NI-0801 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    NI-0801
  • HY-146372
    CXCR4 antagonist 5
    		Antagonist
    CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately.
    CXCR4 antagonist 5
  • HY-182774
    YU241279
    		Inhibitor 99.58%
    YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma.
    YU241279
  • HY-RS03403
    CXCR3 Human Pre-designed siRNA Set A
    		Inhibitor

    CXCR3 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CXCR3 Human 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-P1949A
    Cyclic MKEY TFA
    		98.47%
    Cyclic MKEY TFA is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY TFA also protects against stroke-induced brain injury in mice.
    Cyclic MKEY TFA
  • HY-P991753
    Anti-Mouse CCL5 Antibody (R6G9)
    		Inhibitor
    Anti-Mouse CCL5 Antibody (R6G9) reacts with mouse CCL5 that can neutralize CCL5 both in vitro and in vivo. Recommend Isotype Controls: Mouse IgG1 kappa, Isotype Control (HY-P99977).
    Anti-Mouse CCL5 Antibody (R6G9)
  • HY-110099
    (±)-NBI-74330
    		Antagonist 99.12%
    (±)-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.
    (±)-NBI-74330
  • HY-P991795
    Anti-Mouse/Human CXCL12 Antibody (K15C)
    		Inhibitor
    Anti-Mouse/Human CXCL12 Antibody (K15C) reacts with mouse CXCL12. Anti-Mouse/Human CXCL12 Antibody (K15C) has the effect of neutralizing CXCL12/SDF-1 both in vivo and in vitro. Recommend Isotype Controls: Mouse IgG2a kappa, Isotype Control (HY-P99978).
    Anti-Mouse/Human CXCL12 Antibody (K15C)
  • HY-RS03400
    CXCR2 Human Pre-designed siRNA Set A
    		Inhibitor

    CXCR2 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CXCR2 Human Pre-designed siRNA Set A
  • HY-18263A
    Elubrixin
    		Antagonist
    Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
    Elubrixin
  • HY-120878A
    (R,R)-CXCR2-IN-2
    		Antagonist 99.37%
    (R,R)-CXCR2-IN-2 (compound 67), diastereoisomer of CXCR2-IN-2 (compound 68) (HY-120878), is a CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
    (R,R)-CXCR2-IN-2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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