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-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
    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-P991477
    HFB-100204
    Inhibitor
    HFB-100204 is a human monoclonal antibody (mAb) targeting CXCR5. HFB-100204 reduces CXCR5+ immune cells, including B cells and Tfh cells, in the blood and spleen of hCXCR5 knockout mice. HFB-100204 can be used in autoimmune diseases research.
    HFB-100204
  • 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-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-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-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-162632
    Hit 14
    Inhibitor
    Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC50 of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models.
    Hit 14
  • 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
  • HY-RS03399
    Cxcr1 Rat Pre-designed siRNA Set A
    Inhibitor

    Cxcr1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Cxcr1 Rat Pre-designed siRNA Set A
    Cxcr1 Rat Pre-designed siRNA Set A
  • HY-173404
    VB-85247
    Inducer
    VB-85247 is a STING agonist. VB-85247 induces upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as maturation and activation of dendritic cells by activating the STING pathway. VB-85247 can achieve regression of intrabladder tumors and can be used in bladder cancer research.
    VB-85247
  • HY-144783
    CXCR2 antagonist 6
    Antagonist
    CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].
    CXCR2 antagonist 6
  • HY-RS03398
    Cxcr1 Mouse Pre-designed siRNA Set A
    Inhibitor

    Cxcr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cxcr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Cxcr1 Mouse Pre-designed siRNA Set A
    Cxcr1 Mouse Pre-designed siRNA Set A
  • HY-P1102A
    TC14012 TFA
    Modulator
    TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity.
    TC14012 TFA
  • HY-139906
    CXCL12 ligand 1
    Agonist
    CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12.
    CXCL12 ligand 1
  • HY-101407R
    Nicotinamide N-oxide (Standard)
    Antagonist
    Nicotinamide N-oxide (Standard) is the analytical standard of Nicotinamide N-oxide. This product is intended for research and analytical applications. Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
    Nicotinamide N-oxide (Standard)
  • HY-144781
    CXCR2 antagonist 5
    Antagonist
    CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM)[ 1].
    CXCR2 antagonist 5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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