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 (173)
Related Products (173)
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VB-85247
0 ImagesCat. No.: HY-173404VB-85247 is a STING agonist. VB-85247 induces upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as maturation and activation of dendritic cells by activating the STING pathway. VB-85247 can achieve regression of intrabladder tumors and can be used in bladder cancer research.
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Anti-Mouse CXCR2 Antibody (Cx2Mab-1)
0 ImagesCat. No.: HY-P991746Anti-Mouse CXCR2 Antibody (Cx2Mab-1) reacts with mouse CXCR2 targeting the N-terminal extracellular domain of CXCR2. Recommend Isotype Controls: Rat IgG2b kappa, Isotype Control (HY-P990682).
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AMD 3465 (Standard)
0 ImagesCat. No.: HY-15971ARCAS No.: 185991-24-6Synonyms: GENZ-644494 (Standard)AMD 3465 (Standard) is the analytical standard of AMD 3465. This product is intended for research and analytical applications. 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.
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CXCL12 ligand 1
0 ImagesCat. No.: HY-139906CAS No.: 2045891-59-4CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12.
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Decursin (Standard)
0 ImagesDecursin (Standard) is the analytical standard of Decursin. This product is intended for research and analytical applications. Decursin ((+)-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[4].
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SDF-1α (human)
0 ImagesCat. No.: HY-P4911CAS No.: 1268129-65-2SDF-1α (human) 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) can be used in cardiovascular disease research.
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(R)-SCH 546738
0 Images(R)-SCH 546738 is the R-isomer of SCH 546738 (HY-10017). SCH 546738 is an orally active and non-competitive antagonist for CXCR3 with Ki of 0.4 nM for human CXCR3 receptor.
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CXCR4-IN-2
0 ImagesCat. No.: HY-149558CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis.
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SFB-AMD3465
0 ImagesCat. No.: HY-158317CAS No.: 2416231-90-6
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STING-IN-18
0 ImagesCat. No.: HY-181057STING-IN-18 is an orally active STING inhibitor. STING-IN-18 exhibits an IC50 of 86 nM against STING in murine RAW-LuciaTM ISG cells. STING-IN-18 inhibits STING activation and blocks downstream signaling pathways. STING-IN-18 suppresses kidney injury and inflammation. STING-IN-18 can be used for the research of autoimmune and inflammatory diseases.
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ACT-672125
0 ImagesCat. No.: HY-153240CAS No.: 1449367-94-5ACT-672125 is a potent CXCR3 antagonist with IC50 value of 239 nM in human blood. ACT-672125 has activity for hERG with IC50 value of 18μM. ACT-672125 can be used for the research of autoimmune diseases.
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VUF11211
0 ImagesCat. No.: HY-119208CAS No.: 906556-51-2VUF11211 is an allosteric inverse CXCR3 agonist with a Kd of 0.65 nM.
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BMS-986184
0 ImagesCat. No.: HY-P992047BMS-986184 is a fully human monoclonal antibody targeting interferon gamma-induced protein 10 (IP-10)/CXCL10. BMS-986184 can be used for the research of lupus nephritis.
