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-147808
    CXCR4 antagonist 7
    		Antagonist
    CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome.
    CXCR4 antagonist 7
  • HY-159582
    ACKR3 agonist 1
    		Agonist
    ACKR3 agonist 1 (compound 27) is a selective ACKR3 agonist (EC50=69 nM, Emax=82%) that inhibits platelet aggregation. ACKR3 agonist 1 is metabolically stable and non-cytotoxic, and has the potential to inhibit platelet-mediated thrombosis.
    ACKR3 agonist 1
  • HY-P992476
    TJX7
    		Inhibitor
    TJX7 is a recombinant antibody targeting CXCL13/BCA-1/BLC.
    TJX7
  • HY-19867
    Burixafor
    		Antagonist
    Burixafor (TG-0054) is a potent CXCR4 antagonist with a pIC50 of 7.4. Burixafor inhibits the binding of CXCL12 to CXCR4, antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, and blocks the downstream Gαᵢ-mediated inhibitory effect on cAMP signal transduction. Burixafor mobilizes CD34+ hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor can be used for research on autologous hematopoietic stem cell transplantation (ASCT).
    Burixafor
  • HY-158036
    PROTAC STING Degrader-2
    		Inhibitor
    PROTAC STING Degrader-2 is a STING PROTAC degrader with a DC50 of 0.53 μM. PROTAC STING Degrader-2 reduces the phosphorylation levels of TBK1 and IRF3. PROTAC STING Degrader-2 decreases the mRNA expression levels of IFN-β, CXCL10 and TNF-α, and blocks luciferase secretion. PROTAC STING Degrader-2 can be used in the research of autoimmune diseases.
    PROTAC STING Degrader-2
  • HY-173491
    CXCR2/CCR7 antagonist-1
    		Antagonist
    CXCR2/CCR7 antagonist-1 (compound 6) is a potent CXCR2 and CCR7 dual antagonist with IC50s of 0.0046 and 0.0014 μM, respectively. CXCR2/CCR7 antagonist-1 can be used in the study of cancer metastasis and autoimmune diseases.
    CXCR2/CCR7 antagonist-1
  • HY-164682
    AMD 3329 octahydrobromide
    		Inhibitor
    AMD 3329 octahydrobromide is a potent and selective anti-HIV-1 and HIV-2 compound with activity to inhibit viral replication. AMD 3329 blocks viral invasion by binding to the chemokine receptor CXCR4. AMD 3329 exhibits EC50 values as low as 0.8 and 1.6 nM when inhibiting HIV-1 and HIV-2 replication, showing better antiviral efficacy than AMD3100. AMD 3329 significantly inhibits the binding of specific CXCR4 monoclonal antibodies and the Ca(2+) flux induced by SDF-1alpha. AMD 3329 is also able to effectively interfere with virus-induced syncytium formation, with an EC50 value of 12 nM.
    AMD 3329 octahydrobromide
  • HY-RS03408
    Cxcr4 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cxcr4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr4 Rat Pre-designed siRNA Set A
  • HY-144784
    CXCR2 antagonist 7
    		Antagonist
    CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].
    CXCR2 antagonist 7
  • HY-178205
    BPRCX807
    		Antagonist
    BPRCX 807 is a selective and potent CXCR4 (CXC chemokine receptor type 4) antagonist. BPRCX 807 inhibits CXCL12-mediated ERK and Akt phosphorylation. BPRCX 807 can significantly suppress primary tumor growth. BPRCX 807 can be used for the study of hepatocellular carcinoma.
    BPRCX807
  • HY-181484
    STING agonist-50
    		Activator
    STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer.
    STING agonist-50
  • HY-P5297
    DOTA-CXCR4-L
    		Inhibitor
    DOTA-CXCR4-L is a CXCR4 targeting peptide. DOTA-CXCR4-L can be used in the study of cancers, including glioblastoma and triple-negative breast cancer. NODAGA-LM3 can be labeled with [68Ga]/[177Lu] for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA-CXCR4-L
  • HY-133151
    CXCR6 antagonist 1
    		Antagonist
    CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma.
    CXCR6 antagonist 1
  • HY-113730
    VUF5834
    		Antagonist
    VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
    VUF5834
  • HY-P4810
    Polyphemusin II-Derived Peptide
    		Inhibitor
    Polyphemusin II-Derived Peptide (T140), a CXCR4 inhibitor, shows high inhibitory activity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4.
    Polyphemusin II-Derived Peptide
  • HY-147129
    cGAS-IN-9
    		Inhibitor
    cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC50 values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC50 of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases.
    cGAS-IN-9
  • HY-114366
    BC-1485
    		Inhibitor
    BC-1485 is a small molecule inhibitor of Fibrosis-inducing E3 ligase 1 (FIEL1). BC-1485 protects PIAS4 from ubiquitin-mediated degradation. BC-1485 decreases α-SMA, BAL and CXCL1. BC-1485 ameliorates fibrotic lung injury in murine models.
    BC-1485
  • HY-P11728
    Peptide E5
    		Antagonist
    Peptide E5 is an antagonist targeting the CXCR4/CXCL12 axis. Peptide E5 blocks the CXCR4/CXCL12 axis, downregulates CXCR4 expression, and inhibits the phosphorylation of downstream Akt and Erk. Peptide E5 induces apoptosis, suppresses migration and adhesion of breast cancer cells. Peptide E5 inhibits CXCL12-mediated endothelial progenitor cell recruitment, thereby suppressing tumor angiogenesis. Peptide E5 is applicable to relevant research on breast cancer.
    Peptide E5
  • HY-153464
    CXCR4-IN-1
    		Inhibitor
    CXCR4-IN-1 (Example C5) is a CXCR4 inhibitor (IC50: 20 nM). CXCR4-IN-1 can be used for research of cancer, HIV, diabetic retinopathy, inflammation, etc.
    CXCR4-IN-1
  • HY-P1103A
    CTCE-9908 TFA
    		Antagonist
    CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
    CTCE-9908 TFA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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