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-P991567
    VX5
    		Modulator
    VX5 (VX5/5261) 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. VX5 can be used to study autoimmune diseases like multiple sclerosis and arthritis, and cancers like gastric lymphomas and colon cancer.
    VX5
  • HY-160041A
    Olaptesed pegol sodium
    		Inhibitor
    Olaptesed pegol (NOX-A12) sodium is a L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol sodium neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment. Olaptesed pegol sodium can enhances the infiltration of human primary T cells and NK cells and inhibit tumor growth companied with anti-PD-1 antibody. Olaptesed pegol sodium can be used for researches of colon cancer and lymphocytic leukemia.
    Olaptesed pegol sodium
  • HY-15971
    AMD 3465 hexahydrobromide
    		Antagonist 98.0%
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
    AMD 3465 hexahydrobromide
  • HY-120878
    CXCR2-IN-2
    		Antagonist 99.52%
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
    CXCR2-IN-2
  • HY-15319B
    AMG 487 (S-enantiomer)
    		Antagonist 99.94%
    AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
    AMG 487 (S-enantiomer)
  • HY-112154
    CXCR7 modulator 2
    		Modulator 98.71%
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
    CXCR7 modulator 2
  • HY-101022
    CXCR2-IN-1
    		Inhibitor 99.54%
    CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.
    CXCR2-IN-1
  • HY-147392
    CXCR2 antagonist 8
    		Antagonist 98.38%
    CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research.
    CXCR2 antagonist 8
  • HY-128063
    CXCR3 antagonist 1
    		Antagonist 98.6%
    CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC50=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes).
    CXCR3 antagonist 1
  • HY-139643A
    CXCR7 antagonist-1 hydrochloride
    		Antagonist 99.41%
    CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases.
    CXCR7 antagonist-1 hydrochloride
  • HY-165428
    SCH-900875
    		Inhibitor 98.16%
    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-P990737
    Eltrekibart
    		98.00%
    Eltrekibart is an anti-CXCL human IgG4 κ monoclonal antibody. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).
    Eltrekibart
  • HY-160041
    Olaptesed pegol
    		Inhibitor
    Olaptesed pegol (NOX-A12) is a L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment. Olaptesed pegol can enhances the infiltration of human primary T cells and NK cells and inhibit tumor growth companied with anti-PD-1 antibody. Olaptesed pegol can be used for researches of colon cancer and lymphocytic leukemia.
    Olaptesed pegol
  • HY-107987
    CXCR7 modulator 1
    		Modulator 99.27%
    CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
    CXCR7 modulator 1
  • HY-16981
    SB-332235
    		Antagonist 98.7%
    SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells.
    SB-332235
  • HY-13696
    MSX-122
    		Antagonist 98.16%
    MSX-122 is an orally active partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 has anti-inflammatory and anti-metastatic activity.
    MSX-122
  • HY-P7061A
    ALX 40-4C Trifluoroacetate
    		Inhibitor 99.78%
    ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
    ALX 40-4C Trifluoroacetate
  • HY-P1103
    CTCE-9908
    		Antagonist 99.54%
    CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
    CTCE-9908
  • HY-16509
    UNBS5162
    		Antagonist 99.07%
    UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
    UNBS5162
  • HY-P10333A
    LIH383 TFA
    		Agonist 99.83%
    LIH383 TFA is an agonist of ACKR3 (CXCR7) (EC50=0.61 nM). LIH383 TFA efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.
    LIH383 TFA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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