CXCR
CXC chemokine receptors (CXCRs) are seven-transmembrane chemokine receptors that regulate immune-system development and leukocyte trafficking through chemokine-directed cell migration[1]. Mechanistically, CXCR signaling connects ligand recognition to immune-cell positioning, with CXCL8-CXCR1/CXCR2 driving neutrophil chemotaxis during infection and tissue injury[2]. In disease and experimental models, CXCR4 binds CXCL12/SDF-1, supports chemotaxis and calcium signaling, and functions as the HIV-1 entry cofactor LESTR/fusin[3]. Compared with related isoforms, CXCR3-A and CXCR3-B show divergent activities: CXCR3-B mediates endothelial growth inhibition induced by CXCL9, CXCL10, CXCL11, and CXCL4[4]. CXCR5 differs functionally by mediating selective B-lymphocyte attraction through BCA-1/CXCL13, linking this receptor to lymphoid-tissue B-cell trafficking[5]. For experimental applications, plerixafor/AMD3100 provides a validated CXCR4 antagonist tool that rapidly mobilizes CD34⁺ hematopoietic cells in healthy volunteers[6].
References:
- [1]. Bachelerie F, et al. International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev. 2013 Nov 11;66(1):1-79. [Content Brief]
- [2]. Cambier S, et al. The chemokines CXCL8 and CXCL12: molecular and functional properties, role in disease and efforts towards pharmacological intervention. Cell Mol Immunol. 2023 Mar;20(3):217-251. [Content Brief]
- [3]. Bleul CC, et al. The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/fusin and blocks HIV-1 entry. Nature. 1996 Aug 29;382(6594):829-33. [Content Brief]
- [4]. Lasagni L, et al. An alternatively spliced variant of CXCR3 mediates the inhibition of endothelial cell growth induced by IP-10, Mig, and I-TAC, and acts as functional receptor for platelet factor 4. J Exp Med. 2003;197(11):1537-49. [Content Brief]
- [5]. Legler DF, et al. B cell-attracting chemokine 1, a human CXC chemokine expressed in lymphoid tissues, selectively attracts B lymphocytes via BLR1/CXCR5. J Exp Med. 1998 Feb 16;187(4):655-60. [Content Brief]
- [6]. Devine SM, et al. Rapid mobilization of CD34+ cells following administration of the CXCR4 antagonist AMD3100 to patients with multiple myeloma and non-Hodgkin's lymphoma. J Clin Oncol. 2004;22(6):1095-102. [Content Brief]
All Product Categories
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CXCR Related Products (168)
Related Products (168)
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Pentixafor
0 ImagesPentixafor is a peptide that targets CXCR4. Pentixafor is capable of being labelled with 68Gallium (68Ga) for positron emission tomography (PET) imaging. Pentixafor can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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Kynurenic acid (Standard)
0 ImagesSynonyms: Quinurenic acid (Standard)Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. 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.
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Decursin
0 ImagesDecursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities.
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ML 145
0 ImagesCat. No.: HY-107536CAS No.: 1164500-72-4
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UNBS5162
0 ImagesUNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
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PD-1/PD-L1-IN-63
0 ImagesPD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma.
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YU241279
0 ImagesYU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma.
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Baminercept
0 ImagesSynonyms: BG 9924; TT-47Baminercept (BG 9924; TT-47) is an Ig fusion protein targeting the lymphotoxin β receptor (LTβR). Baminercept effectively regulates subsets of circulating immune cells by inhibiting LIGHT, LT-α1β2 and their receptors. Baminercept also increases blood lymphocyte counts and reduces plasma CXCL13 levels. Baminercept carries a high risk of hepatotoxicity. Baminercept can be used in research on rheumatoid arthritis and primary Sjögren's syndrome.
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Eldelumab
0 ImagesSynonyms: BMS-936557; MDX-1100Eldelumab (BMS-936557) is a human anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease.
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Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5)
0 ImagesCat. No.: HY-P990255Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) is an anti-mouse CXCL9/MIG IgG monoclonal antibody. Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can reduce tumor infiltration of CD8+ cytotoxic T cells (CTLs). Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can prolong the survival of transplanted hearts. Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can be used for researches on immunology and cancer such as prostate cancer.
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SDF-1α (human) TFA
0 ImagesCat. No.: HY-P4911APurity: 98.89%SDF-1α (human) TFA is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) TFA can be used in cardiovascular disease research.
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ATI-2341 TFA
0 ImagesCat. No.: HY-P0172APurity: 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).
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(Rac)-Reparixin
0 ImagesSynonyms: (Rac)-Repertaxin; (Rac)-DF 1681Y
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TFAM activator 1
0 ImagesTFAM 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.
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Quetmolimab
0 ImagesSynonyms: E6011Quetmolimab (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.
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CXCL8 (54-72)
0 ImagesCat. No.: HY-P10300Purity: 99.90%Synonyms: IL-8 (54-72)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.
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Anti-Mouse CXCL10 Antibody (1F11)
0 ImagesCat. No.: HY-P991761Anti-Mouse CXCL10 Antibody (1F11) is a mouse CXCL10 antibody. Anti-Mouse CXCL10 Antibody (1F11) blocks the activity of CXCL10 and inhibits GPCR-dependent interstitial motility of Th1 cells in inflamed dermis. Anti-Mouse CXCL10 Antibody (1F11) can be used for research on inflammation-related diseases. Recommended isotype control: Polyclonal Armenian hamster IgG, Isotype Control (HY-P990305).
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VX5
0 ImagesCat. No.: HY-P991567Synonyms: VX5/5261VX5 (VX5/5261) is a humanized IgG1κ monoclonal antibody inhibitor targeting BCA-1/CXCL13. VX5 significantly inhibits human CXCL13-mediated internalization of CXCR5, blocks both human and mouse CXCL13-dependent B-cells chemotaxis and migration. VX5 can be used to study autoimmune diseases like multiple sclerosis and arthritis, and cancers like gastric lymphomas and colon cancer.
