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. 상품명 효과 Purity Chemical Structure
  • HY-P0172A
    ATI-2341 TFA
    		Agonist 98.08%
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
    ATI-2341 TFA
  • HY-N7688
    Regaloside B
    		99.90%
    Regaloside B is a phenylpropane. Regaloside B can be isolated from Lilium longiflorum. Regaloside B can inhibit the expression of VCAM-1, iNOS, and COX-2, with a p-p65/p-65 ratio. Regaloside B inhibits the mRNA of various chemokines and angiogenic factors (CXCL9, CXCL10, IL8, IDO). Regaloside B has anti-inflammatory activity. Regaloside B can be used for osteogenic differentiation research.
    Regaloside B
  • HY-B0770
    Artemotil
    		98.0%
    Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
    Artemotil
  • HY-P1104A
    FC131 TFA
    		Antagonist 99.87%
    FC131 TFA is a CXCR4 antagonist, inhibits [125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
    FC131 TFA
  • HY-122822
    GSK699
    		Inhibitor 98.80%
    GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases.
    GSK699
  • HY-100677
    VUF11207
    		Agonist 99.98%
    VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
    VUF11207
  • HY-P10300
    CXCL8 (54-72)
    		99.90%
    CXCL8 (54-72) is a C-terminal peptide based on the chemokine CXCL8. CXCL8 (54-72) has an interaction between a long and highly positively charged C-terminal region and a negative charge on the GAG that binds to the GAG. CXCL8 (54-72) can inhibit the adhesion and migration of neutrophils and adhesion of endothelial cells. CXCL8 (54-72) can be used to study chemokines in inflammatory response.
    CXCL8 (54-72)
  • HY-15251A
    (Rac)-Reparixin
    		Control 99.75%
    (Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    (Rac)-Reparixin
  • HY-12927
    SX-517
    		Antagonist 99.90%
    SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model.
    SX-517
  • HY-50101C
    Mavorixafor hydrochloride
    		Antagonist 99.64%
    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-P99404
    Quetmolimab
    		Inhibitor 99.9%
    Quetmolimab (E6011) is a humanized anti-Fractalkine (CX3CL1) monoclonal antibody. Quetmolimab binds to membrane-bound and soluble Fractalkine, neutralizes Fractalkine-induced migration of CX3CR1-expressing cells, mediates target-bound complex elimination from serum. Quetmolimab suppresses free soluble Fractalkine levels in cynomolgus monkeys, with target engagement linked to increased serum total Fractalkine concentration. Quetmolimab can be used for the research of Crohn’s disease, rheumatoid arthritis, and primary biliary cholangitis.
    Quetmolimab
  • HY-D0976
    NF279
    		Antagonist 98.5%
    NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC50 value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection.
    NF279
  • HY-15971A
    AMD 3465
    		Antagonist 98.24%
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
    AMD 3465
  • HY-19867A
    Burixafor hydrobromide
    		Antagonist
    Burixafor (TG-0054) hydrobromide is a potent CXCR4 antagonist with a pIC50 of 7.4. Burixafor hydrobromide inhibits the binding of CXCL12 to CXCR4, antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, and blocks the downstream Gαᵢ-mediated inhibitory effect on cAMP signal transduction. Burixafor hydrobromide mobilizes CD34+ hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor hydrobromide can be used for research on autologous hematopoietic stem cell transplantation (ASCT).
    Burixafor hydrobromide
  • HY-19519A
    Ladarixin sodium
    		Antagonist 99.84%
    Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma.
    Ladarixin sodium
  • HY-10011
    SCH 563705
    		Antagonist 99.86%
    SCH 563705 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.
    SCH 563705
  • HY-111793
    NUCC-390
    		Agonist 98.01%
    NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo.
    NUCC-390
  • HY-175739
    TFAM activator 1
    		Inhibitor 99.25%
    TFAM activator 1 is a TFAM activator. TFAM activator 1 increases TFAM protein levels, promotes mitochondrial DNA stability, increases mitochondrial DNA copy number, and prevents mitochondrial DNA from escaping into the cytoplasm. TFAM activator 1 improves cellular energy metabolism in cybrid cells. TFAM activator 1 reduces fibrosis markers in fibroblasts. TFAM activator 1 can be used in the research of mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes syndrome, systemic sclerosis, and autoimmune diseases.
    TFAM activator 1
  • HY-P10415
    EPI-X4
    		Antagonist 98.91%
    EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM.
    EPI-X4
  • HY-18263C
    Elubrixin tosylate
    		Antagonist 98.14%
    Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
    Elubrixin tosylate
Cat. No. 상품명 / Synonyms Species Source
Cat. No. 상품명 / Synonyms Application Reactivity
CXCR Isoform Comparison

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