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-101033
    GPR35 agonist 1
    99.22%
    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good agentgability.
    GPR35 agonist 1
  • 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-12927
    SX-517
    Antagonist 99.88%
    SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model.
    SX-517
  • HY-120878A
    (R,R)-CXCR2-IN-2
    Antagonist 99.37%
    (R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant 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
  • HY-103009
    MSX-127
    Antagonist 99.68%
    MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
    MSX-127
  • HY-103010
    MSX-130
    Antagonist 98.00%
    MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
    MSX-130
  • HY-15971A
    AMD 3465
    Antagonist
    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-145640
    Vimnerixin
    Antagonist 99.39%
    Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease.
    Vimnerixin
  • 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-P99404
    Quetmolimab
    Inhibitor
    Quetmolimab is a humanized anti-CX3CL1 monoclonal antibody. However, CX3CL1 is a chemokine with a modulating effect on chemotaxis and adhesion.
    Quetmolimab
  • 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-101458
    IT1t
    Antagonist
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
    IT1t
  • HY-10011
    SCH 563705
    Antagonist 99.29%
    SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
    SCH 563705
  • HY-P7061
    ALX 40-4C
    Inhibitor
    ALX 40-4C 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
  • HY-111793
    NUCC-390
    Agonist
    NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo.
    NUCC-390
  • HY-111149
    PS372424
    Agonist
    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.
    PS372424
  • HY-P3612
    CTCE-0214
    Agonist 98.94%
    CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research.
    CTCE-0214
  • HY-50101
    Mavorixafor
    Antagonist
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
    Mavorixafor
  • 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-15319B
    AMG 487 (S-enantiomer)
    Antagonist 99.81%
    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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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