1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

CXCR

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

  • CXCR1

  • CXCR2

  • CXCR3

  • CXCR4

  • CXCR7

  • CX3CR1

CXCR Related Products (34):

Cat. No. Product Name Effect Purity
  • HY-10046
    Plerixafor Antagonist >98.0%
    Plerixafor is a selective CXCR4 antagonist with an IC50 of 44 nM.
  • HY-50912
    Plerixafor octahydrochloride Antagonist 98.90%
    Plerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.
  • HY-15251
    Reparixin Inhibitor 99.88%
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-10198
    Navarixin Antagonist 99.06%
    Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
  • HY-15319
    AMG 487 Inhibitor 99.65%
    AMG 487 is an antagonist of the chemokine receptor CXCR3, which inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 with IC50 values of 8.0 and 8.2 nM, respectively.
  • HY-P7061A
    ALX 40-4C Trifluoroacetate Inhibitor 98.15%
    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.
  • HY-112154
    CXCR7 modulator 2 Modulator
    CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), with a Ki of 13 nM.
  • HY-107456
    E6130 Modulator
    E6130 is an orally available and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
  • HY-15252
    Reparixin L-lysine salt Inhibitor 98.44%
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
  • HY-12488
    LY2510924 Inhibitor >98.0%
    LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
  • HY-16711
    SB225002 Antagonist 99.58%
    SB225002 is a potent and selective CXCR2 antagonist with an IC50 of 22 nM.
  • HY-19855
    AZD-5069 Antagonist 98.97%
    AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
  • HY-10017
    SCH 546738 Antagonist 99.20%
    SCH 546738 is a novel, potent and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
  • HY-13406
    TAK-779 Antagonist 99.73%
    TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
  • HY-19768
    Danirixin Antagonist 98.23%
    Danirixin is a selective, and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8.
  • HY-P0171
    BKT140 4-fluorobenzoyl Antagonist 99.19%
    BKT140 4-fluorobenzoyl is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM. Sequence: 4F-Benzoyl-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-Lys-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge: Cys4-Cys13).
  • HY-50101A
    AMD-070 hydrochloride Antagonist >98.0%
    AMD-070 hydrochloride 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.
  • HY-13848
    AZD8797 Antagonist 98.22%
    AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
  • HY-13696
    MSX-122 Antagonist 99.74%
    MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
  • HY-10011
    SCH 563705 Antagonist
    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.
Isoform Specific Products

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