2. GPCR/G Protein
    Immunology/Inflammation
  3. 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 (229):

Cat. No. Product Name Effect Purity
  • HY-15251
    Reparixin Inhibitor 99.99%
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-10046
    Plerixafor Antagonist
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
  • HY-15319
    AMG 487 Inhibitor 99.80%
    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively[1].
  • HY-16711
    SB225002 Antagonist 99.87%
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
  • HY-100806
    Kynurenic acid 99.21%
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  • 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[1].
  • HY-163480
    PF-06835375 Antagonist
    PF-06835375 is a humanized IgG1 antibody selective against CXCR5 expressed on B cells, Tfh cells, and circulating Tfh-like (cTfh) cells. PF-06835375 can be used for the study of systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001)[1].
  • HY-P991227
    Anti-CD185/CXCR5 Antibody Inhibitor
    Anti-CD185/CXCR5 Antibody is an antibody inhibitor, targeting to human CD185/CXCR5.
  • HY-18263
    Elubrixin hydrochloride Antagonist
    Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation[1][2][3].
  • HY-50101C
    Mavorixafor hydrochloride Antagonist 99.10%
    Mavorixafor (AMD-070) hydrochloride is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor hydrochloride also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 nM and 9 nM, respectively. Mavorixafor hydrochloride can be used for the study of WHIM syndrome[1].
  • HY-16981
    SB-332235 Antagonist 98.7%
    SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells[1][2].
  • HY-P990389
    Anti-CXC-ELR Antibody
    Anti-CXC-ELR Antibody is a human-derived antibody expressed in CHO, targeting CXC-ELR. Anti-CXC-ELR Antibody is equipped with huIgG4SP type heavy chain and huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-CXC-ELR Antibody can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
  • HY-120878
    CXCR2-IN-2 Antagonist 99.52%
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1].
  • HY-P990255
    Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5)
    Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) is a Armenian hamster-derived IgG, κ type antibody inhibitor, targeting to mouse CXCL9/MIG.
  • HY-101458
    IT1t Antagonist
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-142617
    ACT-1004-1239 Antagonist 99.80%
    ACT-1004-1239 is a potent, selective, orally active CXCR7 antagonist with an IC50 value of 3.2 nM[1][2].
  • HY-P990391
    Anti-CXCL4/PF4 Antibody
    The Anti-CXCL4/PF4 Antibody is a human antibody expressed in CHO cells that targets CXCL4/PF4. The Anti-CXCL4/PF4 Antibody has a huIgG4SP type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 144.5 kDa. The isotype control for Anti-CXCL4/PF4 Antibody can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
  • HY-122197
    ML339 Antagonist 99.88%
    ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research[1][2].
  • HY-P990394
    Anti-CXCR3/GPR9/CD183 Antibody 98.45%
    Anti-CXCR3/GPR9/CD183 Antibody is a human-derived antibody expressed in CHO, targeting CXCR3/GPR9/CD183. The Anti-CXCR3/GPR9/CD183 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For the isotype control of Anti-CXCR3/GPR9/CD183 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
  • 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[1].