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 Related Products (25):

Cat. No. Product Name Effect Purity
  • HY-50912
    Plerixafor octahydrochloride Antagonist
    Plerixafor octahydrochloride is a CXCR4 antagonist, the IC50 values for GTP-binding and chemotaxis are 27±2.2 and 51±17 nM, respectively.
  • HY-15251
    Reparixin Inhibitor
    Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
  • HY-10046
    Plerixafor Inhibitor
    Plerixafor is a selective CXCR4 inhibitor with IC50 of 44 nM.
  • HY-10198
    SCH 527123 Antagonist
    SCH 527123 is a potent, allosteric antagonist of both CXCR1 and CXCR2, with IC50 values of 1000 nM and 3-6 nM, respectivelly.
  • HY-15252
    Reparixin L-lysine salt Inhibitor
    Reparixin L-lysine salt is a potent and specific allosteric inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
  • HY-101458
    IT1t Antagonist
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-101407
    Nicotinamide N-oxide Antagonist
    Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
  • HY-P0171
    BKT140 Antagonist
    BKT140 is a novel CXCR4 antagonist with an IC50 value of ~1 nM.
  • HY-50101A
    AMD-070 hydrochloride Antagonist
    AMD-070 (hydrochloride) is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, and inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
  • HY-10017
    SCH 546738 Antagonist
    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-15971
    AMD 3465 hexahydrobromide Antagonist
    AMD 3465 (hexahydrobromide) is a potent, selective CXCR4 antagonist, and inhibits SDF-1α-ligand binding with Ki of 41.7 nM.
  • HY-16711
    SB225002 Antagonist
    SB225002 is a potent and selective CXCR2 antagonist with an IC50 of 22 nM.
  • HY-19768
    Danirixin Antagonist
    Danirixin is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.
  • HY-15319
    AMG 487 Inhibitor
    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-15320
    NBI-74330 Antagonist
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
  • HY-10011
    SCH 563705 Antagonist
    SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist.
  • HY-15478
    WZ811 Antagonist
    WZ811 is a novel small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.
  • HY-13696
    MSX-122 Antagonist
    MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions (IC50 = 10 nM).
  • HY-15462
    SRT3109 Antagonist
    SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
  • HY-13021
    SRT3190 Antagonist
    SRT3190 is CXCR2 ligand.