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-19867A
    Burixafor hydrobromide
    		Antagonist ≥98.0%
    Burixafor (TG-0054) hydrobromide is a selective, orally active CXCR4 antagonist that effectively blocks the interaction between CXCR4 and its ligand, stromal cell-derived factor SDF-1. Burixafor hydrobromide interferes with the SDF-1/CXCR4 signaling pathway, prompting the release of bone marrow stem cells into the peripheral circulation, exerting immunomodulatory and anti-inflammatory activities. Burixafor hydrobromide can be used in the study of cancer, Intraocular neovascular diseases (such as choroidal neovascularization), myocardial infarction and other diseases, with the potential to mobilize stem cells, improve cardiac function and reduce inflammatory responses.
    Burixafor hydrobromide
  • 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-P10300
    CXCL8 (54-72)
    		99.03%
    CXCL8 (54-72) is a C-terminal peptide based on the chemokine CXCL8. CXCL8 (54-72) has an interaction between a long and highly positively charged C-terminal region and a negative charge on the GAG that binds to the GAG. CXCL8 (54-72) can inhibit the adhesion and migration of neutrophils and adhesion of endothelial cells. CXCL8 (54-72) can be used to study chemokines in inflammatory response.
    CXCL8 (54-72)
  • 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-P1104A
    FC131 TFA
    		Antagonist 99.89%
    FC131 TFA is a CXCR4 antagonist, inhibits [125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
    FC131 TFA
  • 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-P990598
    Adakitug
    		≥99.0%
    Adakitug (BMS-986253) is a CHO-expressed human antibody targeting CXCL8/IL-8. Adakitug contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 144.94 kDa. The isotype control for Adakitug can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Adakitug
  • HY-15971A
    AMD 3465
    		Antagonist 99.59%
    AMD 3465 (GENZ-644494) 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
  • HY-112709
    LIT-927
    		99.86%
    LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12 binding to its specific receptor CXCR4 .
    LIT-927
  • HY-P7061A
    ALX 40-4C Trifluoroacetate
    		Inhibitor
    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 99.47%
    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 98.10%
    UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
    UNBS5162
  • HY-P10415
    EPI-X4
    		Antagonist 99.21%
    EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM.
    EPI-X4
  • HY-122891
    SB02024
    		Activator 99.70%
    SB02024 is a potent and orally active VPS34 inhibitor. SB02024 inhibits Vps34 kinase activity. SB02024 induces CCL5 and CXCL10 via STAT1/IRF7. SB02024 shows anticancer activity.
    SB02024
  • HY-114244
    USL311
    		Antagonist 99.97%
    USL311 is a potent and selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
    USL311
  • HY-119259
    AZD8309
    		Antagonist 99.98%
    AZD8309 is an orally active antagonist of CXCR2. AZD8309 has the ability to regulate the transmigration of neutrophils. AZD8309 can be used in the study of inflammatory diseases.
    AZD8309
  • HY-151096
    ACT-660602
    		Antagonist 99.86%
    ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.
    ACT-660602
  • HY-107987
    CXCR7 modulator 1
    		Modulator 99.50%
    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-P990254
    Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173)
    Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173) is a Armenian hamster-derived IgG type antibody inhibitor, targeting to mouse CXCR3/CD183.
    Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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