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-173290
    PDE4D inhibitor 1
    		Inhibitor
    PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.
    PDE4D inhibitor 1
  • HY-RS03410
    CXCR6 Human Pre-designed siRNA Set A
    		Inhibitor

    CXCR6 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CXCR6 Human Pre-designed siRNA Set A
  • HY-P11011
    Peptide R54
    		Antagonist
    Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma.
    Peptide R54
  • HY-RS03402
    Cxcr2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cxcr2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr2 Rat Pre-designed siRNA Set A
  • HY-W104862
    4-Amino-D-phenylalanine
    		Inhibitor 99.74%
    4-Amino-D-phenylalanine ([D-Phe(4-NH2)), a cyclic pentapeptide, inhibits CXCL12 binding to CXCR4 in FC131, with an IC50 of 0.1 μM.
    4-Amino-D-phenylalanine
  • HY-P10971
    Nef-M1
    		Antagonist
    Nef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer.
    Nef-M1
  • HY-139874
    CXCR2 antagonist 3
    		Antagonist
    CXCR2 antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). CXCR2 antagonist 3 demonstrates double-digit nanomolar potencies against CXCR2 and significantly inhibited neutrophil infiltration into the air pouch. CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs and enhance the infiltration of CD3+ T lymphocytes into the Pan02 tumor tissues.
    CXCR2 antagonist 3
  • HY-P991568
    AT009
    		Modulator
    AT009 is an anti-CXCR4 humanized monoclonal antibody. AT009 can be used for cancer research.
    AT009
  • HY-172541
    LN6023 hydrochloride
    		Activator
    LN6023 (hydrochloride) (Compound 27) is a CXCR7 agonist. LN6023 (hydrochloride) induces the recruitment of β-arrestin in HEK293T cells expressing human CXCR7 (EC50 = 3.5 µM). LN6023 (hydrochloride) reduces the surface level of P-selectin in isolated and washed human platelets. LN6023 (hydrochloride) can be used to study platelet-mediated thrombosis.
    LN6023 hydrochloride
  • HY-P10444
    DOTA Conjugated JM#21 derivative 7
    DOTA Conjugated JM#21 derivative 7 (compound Ligand-7) is a derivative of CXCR4 targeting peptide conjugated with DOTA and can be used to produce radioligands. Radiolabeled DOTA Conjugated JM#21 derivative 7, i.e., 177Lu-DOTA, has excellent CXCR4 tumor targeting. In vitro biodistribution results of 177Lu-DOTA showed very low uptake in all non-targeted organs except kidney. DOTA Conjugated JM#21 derivative 7 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
    DOTA Conjugated JM#21 derivative 7
  • HY-P1949
    Cyclic MKEY
    Cyclic MKEY is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY also protects against stroke-induced brain injury in mice.
    Cyclic MKEY
  • HY-RS03405
    Cxcr3 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cxcr3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr3 Rat Pre-designed siRNA Set A
  • HY-168971
    Paeoniflorin-6′-O-benzene sulfonate
    		Antagonist
    Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model.
    Paeoniflorin-6′-O-benzene sulfonate
  • HY-W019787
    BAM-12P
    		Activator
    BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM.
    BAM-12P
  • HY-N0011R
    Baohuoside I (Standard)
    		Inhibitor
    Baohuoside I (Standard) is the analytical standard of Baohuoside I. This product is intended for research and analytical applications. 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 (Standard)
  • HY-RS03412
    Cxcr6 Rat Pre-designed siRNA Set A
    		Inhibitor

    Cxcr6 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cxcr6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Cxcr6 Rat Pre-designed siRNA Set A
  • HY-146413
    HF50731
    		Antagonist
    HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM.
    HF50731
  • HY-P10301
    CXCL9(74-103)
    CXCL9(74-103) is a derivative peptide of CXCL9 that has a high affinity for glycosaminoglycans (GAGs) and can bind to GAGs. CXCL9(74-103) possesses anti-angiogenic properties, capable of reducing EGF, VEGF165, and FGF-2-mediated angiogenesis processes in vitro, without exhibiting cytotoxicity.
    CXCL9(74-103)
  • HY-P10333
    LIH383
    		Agonist
    LIH383 is an agonist of ACKR3 (CXCR7) (EC50=0.61 nM). LIH383 efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.
    LIH383
  • HY-P991647
    ALX-0651
    		Inhibitor
    ALX-0651 is a biparatopic humanized monoclonal antibody inhibitor targeting CXCR4. ALX-0651 inhibits hematopoietic stem cell trafficking, tumor progression and metastasis. ALX-0651 can be used for non-Hodgkin’s lymphoma and multiple myeloma research.
    ALX-0651
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
CXCR Isoform Comparison

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