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 (38):

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 >98.0%
    Plerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.
  • HY-15251
    Reparixin Inhibitor 99.98%
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-15319
    AMG 487 Inhibitor 99.65%
    AMG 487 is an antagonist of chemokine receptor 3 CXCR3 which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
  • HY-10198
    Navarixin Antagonist 98.62%
    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-114244
    USL311 Antagonist 99.97%
    USL311 is a selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  • HY-112709
    LIT-927 99.66%
    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 .
  • HY-19867A
    Burixafor hydrobromide Antagonist
    Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well water soluble anti-angiogenic drug that is of potential value in treating choroid neovascularization. Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction.
  • 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 99.92%
    AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
  • HY-12488
    LY2510924 Inhibitor 99.91%
    LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.
  • HY-15252
    Reparixin L-lysine salt Inhibitor 99.97%
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
  • HY-P0171
    Motixafortide Antagonist 99.19%
    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
  • HY-50101A
    Mavorixafor trihydrochloride Antagonist 98.72%
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 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-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-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-19768
    Danirixin Antagonist 98.21%
    Danirixin is a selective, and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8.
  • HY-N0011
    Baohuoside I Inhibitor 98.96%
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
  • HY-101458A
    IT1t dihydrochloride Antagonist 98.09%
    IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
Isoform Specific Products

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