2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
  4. CXCR

CXCR

CXC chemokine receptors; C-X-C motif chemokine receptors

CXCR

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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 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110269
    VUF 11222
    		Agonist 99.91%
    VUF 11222 (Compound 38) is a CXCR3 non-peptide-like agonist. VUF 11222 can be used in the study of inflammation.
    VUF 11222
  • 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.
    Mavorixafor hydrochloride
  • HY-18263A
    Elubrixin
    		Antagonist
    Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
    Elubrixin
  • HY-120878A
    (R,R)-CXCR2-IN-2
    		Antagonist 99.37%
    (R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
    (R,R)-CXCR2-IN-2
  • HY-101458
    IT1t
    		Antagonist
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
    IT1t
  • HY-P4111
    Peptide R
    		Antagonist
    Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research.
    Peptide R
  • HY-P7061
    ALX 40-4C
    		Inhibitor
    ALX 40-4C 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.
    ALX 40-4C
  • HY-168531
    EMU-116
    		Antagonist
    EMU-116 is an orally active CXCR4 antagonist. EMU-116 can be used in the study of cancer.
    EMU-116
  • HY-10011A
    (S)-SCH 563705
    		Antagonist 99.94%
    (S)-SCH 563705 is a S-enantiomer of SCH 563705. SCH 563705 (compound 16) 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.
    (S)-SCH 563705
  • HY-P4846
    Ac-Pro-Gly-Pro-OH
    		Agonist 99.49%
    Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and can be used as CXCR2 agonist. Ac-Pro-Gly-Pro-OH elicits bactericidal activity and inhibits lung inflammation, reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH enhances the production of type 1 cytokines (IFN-γ and IL-12) but inhibits the production of proinflammatory cytokines. Ac-Pro-Gly-Pro-OH has the potential for the research of sepsis.
    Ac-Pro-Gly-Pro-OH
  • HY-111149
    PS372424
    		Agonist
    PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.
    PS372424
  • 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-RS03403
    CXCR3 Human Pre-designed siRNA Set A
    		Inhibitor

    CXCR3 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CXCR3 Human Pre-designed siRNA Set A
    CXCR3 Human Pre-designed siRNA Set A
  • HY-50101
    Mavorixafor
    		Antagonist
    Mavorixafor (AMD-070) 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 can be used for the study of WHIM syndrome.
    Mavorixafor
  • HY-103010
    MSX-130
    		Antagonist 98.00%
    MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
    MSX-130
  • HY-161735
    CXCR4-IN-3
    		Inhibitor 99.69%
    CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research.
    CXCR4-IN-3
  • HY-122058A
    KRH-3955 hydrochloride
    		Antagonist
    KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
    KRH-3955 hydrochloride
  • HY-RS03406
    CXCR4 Human Pre-designed siRNA Set A
    		Inhibitor

    CXCR4 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CXCR4 Human Pre-designed siRNA Set A
    CXCR4 Human Pre-designed siRNA Set A
  • HY-P1104
    FC131
    		Antagonist
    FC131 is a potent CXCR4 antagonist. FC131 inhibits [125I]-SDF-1 binding to CXCR4 with an IC50 of 4.5 nM. FC131 has anti-HIV activity.
    FC131
  • HY-RS03407
    Cxcr4 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Cxcr4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cxcr4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr4 Mouse Pre-designed siRNA Set A
    Cxcr4 Mouse Pre-designed siRNA Set A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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