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-10046
    Plerixafor
    Antagonist 99.67%
    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.
    Plerixafor
  • 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.
    SB225002
  • HY-15319
    AMG 487
    Inhibitor 99.65%
    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.
    AMG 487
  • HY-15251
    Reparixin
    Inhibitor 99.95%
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin
  • HY-50912
    Plerixafor octahydrochloride
    Antagonist ≥98.0%
    Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
    Plerixafor octahydrochloride
  • HY-163475
    CXCL-CXCR1/2-IN-1
    Inhibitor 99.64%
    CXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects.
    CXCL-CXCR1/2-IN-1
  • HY-P4109A
    vMIP-II (1-21) TFA
    Inhibitor
    vMIP-II (1-21) (NT21MP) TFA is an inhibitor of CXCR4. vMIP-II (1-21) TFA interacts broadly with CC and CXC chemokine receptors. vMIP-II (1-21) TFA inhibits CXCR4 by competing with 125I-SDF-1R for binding sites (IC50=190 nM).
    vMIP-II (1-21) TFA
  • HY-50101C
    Mavorixafor hydrochloride
    Antagonist
    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
  • HY-100806
    Kynurenic acid
    98.58%
    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.
    Kynurenic acid
  • HY-10198
    Navarixin
    Antagonist 98.90%
    Navarixin (SCH 527123) is a potent, allosteric and orally active 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.
    Navarixin
  • HY-13848
    AZD8797
    99.54%
    AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.
    AZD8797
  • HY-19855
    AZD-5069
    Antagonist 99.91%
    AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
    AZD-5069
  • HY-P0171
    Motixafortide
    Antagonist 99.88%
    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
    Motixafortide
  • 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.
    TAK-779
  • HY-119339
    SX-682
    Inhibitor 99.67%
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
    SX-682
  • 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.
    ACT-1004-1239
  • HY-50101A
    Mavorixafor trihydrochloride
    Antagonist 99.75%
    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.
    Mavorixafor trihydrochloride
  • 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 CXCR5CXCR4CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research.
    ML339
  • HY-N0011
    Baohuoside I
    Inhibitor 99.96%
    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.
    Baohuoside I
  • HY-19519
    Ladarixin
    Antagonist 99.76%
    Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma.
    Ladarixin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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