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-101458
    IT1t
    Antagonist
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
    IT1t
  • HY-103009
    MSX-127
    Antagonist 99.68%
    MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
    MSX-127
  • HY-P11011A
    Peptide R54 acetate
    Antagonist
    Peptide R54 acetate (Pep R54 acetate) is a CXCR4 antagonist. Peptide R54 acetate inhibits CXCL12-dependent activation of pERK1/2 and pAKT. The combination of Peptide R54 acetate and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer.
    Peptide R54 acetate
  • HY-168095
    CXCR4 antagonist 10
    Inhibitor
    CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research.
    CXCR4 antagonist 10
  • HY-P4111
    Peptide R
    Antagonist
    Peptide R is a cyclic peptide and a specific CXCR4 antagonist. Peptide R exhibits excellent ability to effectively remodel tumor stroma. Peptide R has potential for use in tumor research.
    Peptide R
  • HY-13021
    SRT3190
    Antagonist 99.77%
    SRT3190 is an antagonist of CXCR2, used in the research of chemokine mediated diseases.
    SRT3190
  • HY-P4111A
    Peptide R TFA
    Antagonist 98.34%
    Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research.
    Peptide R TFA
  • HY-162632
    Hit 14
    Inhibitor ≥99.0%
    Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC50 of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models.
    Hit 14
  • HY-P991752
    Anti-Mouse CXCL16 Antibody (12-81)
    Inhibitor
    Anti-Mouse CXCL16 Antibody (12-81) reacts with the extracellular domain of CXCL16. Anti-Mouse CXCL16 Antibody (12-81) can neutralize CXCL16/SR-PSOX both in vitro and in vivo. Recommend Isotype Controls: Rat IgG1 kappa, Isotype Control (HY-P99979).
    Anti-Mouse CXCL16 Antibody (12-81)
  • HY-101407R
    Nicotinamide N-oxide (Standard)
    Antagonist
    Nicotinamide N-oxide (Standard) is the analytical standard of Nicotinamide N-oxide. This product is intended for research and analytical applications. Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
    Nicotinamide N-oxide (Standard)
  • HY-P10973
    Peptide R analogue 10
    Antagonist
    Peptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer.
    Peptide R analogue 10
  • 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-147979
    CXCR4 antagonist 9
    Antagonist
    CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM.
    CXCR4 antagonist 9
  • HY-146054
    CXCR4 modulator-2
    Modulator
    CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model.
    CXCR4 modulator-2
  • HY-123813A
    CCX-777 formic
    Agonist 98.01%
    CCX-777 formic is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 formic induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 formic functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 formic is widely used in cancer-related research.
    CCX-777 formic
  • HY-147978
    CXCR4 antagonist 8
    Antagonist
    CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration.
    CXCR4 antagonist 8
  • 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-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-163480
    PF-06835375
    Antagonist
    PF-06835375 is a selective, humanized CXCR5-targeting immunoglobulin G1 antibody. PF-06835375 depletes CXCR5-positive B cells, follicular helper T cells and circulating Tfh-like cells. PF-06835375 is applicable to research related to autoimmune diseases.
    PF-06835375
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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