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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CXCR4 antagonist 2
0 ImagesCat. No.: HY-132936CAS No.: 2243636-57-7CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
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SQA1
0 ImagesCat. No.: HY-162505CAS No.: 1255915-27-5
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Anti-CXCL4/PF4 Antibody
0 ImagesCat. No.: HY-P990391The Anti-CXCL4/PF4 Antibody is a human antibody expressed in CHO cells that targets CXCL4/PF4. The Anti-CXCL4/PF4 Antibody has a huIgG4SP type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 144.5 kDa. The isotype control for Anti-CXCL4/PF4 Antibody can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
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Benzoylpaeoniflorin (Standard)
0 ImagesCat. No.: HY-N0852RCAS No.: 38642-49-8Benzoylpaeoniflorin (Standard) is an analytical standard for Benzoylpaeoniflorin (HY-N0852). This product is intended for research and analytical applications. Benzoylpaeoniflorin is an orally active monoterpene glycoside compound. Benzoylpaeoniflorin exerts anti-inflammatory, anti-allergic, psoriasis-improving and sepsis-improving effects by inhibiting signaling pathways such as TNF/NF-κB and MAPK, as well as regulating immune homeostasis. Benzoylpaeoniflorin can be used in research related to immune, allergic and inflammatory diseases.
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HFB-100204
0 ImagesCat. No.: HY-P991477HFB-100204 is a human monoclonal antibody (mAb) targeting CXCR5. HFB-100204 reduces CXCR5+ immune cells, including B cells and Tfh cells, in the blood and spleen of hCXCR5 knockout mice. HFB-100204 can be used in autoimmune diseases research.
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CXCR2-IN-1 (Standard)
0 ImagesCat. No.: HY-101022RCAS No.: 1873376-49-8CXCR2-IN-1 (Standard) is the analytical standard of CXCR2-IN-1 (HY-101022). This product is intended for research and analytical applications. CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.
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Plerixafor octahydrochloride (Standard)
0 ImagesSynonyms: AMD3100 octahydrochloride (Standard); JM3100 octahydrochloride (Standard); SID791 octahydrochloride (Standard)Plerixafor (octahydrochloride) (Standard) is the analytical standard of Plerixafor (octahydrochloride). This product is intended for research and analytical applications. Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
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VUF11207 fumarate (Standard)
0 ImagesCat. No.: HY-110318RCAS No.: 1785665-61-3VUF11207 fumarate (Standard) is the analytical standard of VUF11207 (fumarate) (HY-110318). This product is intended for research and analytical applications. VUF11207 fumarate is a CXCR7 agonist that binds specifically to CXCR7. VUF11207 fumarate reduces CXCL12-mediated osteoclastogenesis and bone resorption by inhibiting ERK phosphorylation.
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MSX-127 (Standard)
0 ImagesCat. No.: HY-103009RCAS No.: 6616-56-4
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(Rac)-Reparixin (Standard)
0 ImagesCat. No.: HY-15251ARCAS No.: 957407-64-6Synonyms: (Rac)-Repertaxin (Standard); (Rac)-DF 1681Y (Standard)(Rac)-Reparixin (Standard) is the analytical standard of (Rac)-Reparixin. This product is intended for research and analytical applications. (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.
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ML 145 (Standard)
0 ImagesCat. No.: HY-107536RCAS No.: 1164500-72-4ML 145 (Standard) is the analytical standard of ML 145 (HY-107536). This product is intended for research and analytical applications. ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.
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SB225002 (Standard)
0 ImagesCat. No.: HY-16711RCAS No.: 182498-32-4
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Kynurenic acid sodium (Standard)
0 ImagesKynurenic acid (sodium) (Standard) is the analytical standard of Kynurenic acid (sodium). This product is intended for research and analytical applications. Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
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Anti-CXCR4/CD184 Antibody
0 ImagesCat. No.: HY-P990395Anti-CXCR4/CD184 Antibody is a CHO-expressed human antibody that targets CXCR4/CD184. The Anti-CXCR4/CD184 Antibody has a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-CXCR4/CD184 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
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PF-06465469 (Standard)
0 ImagesCat. No.: HY-108691RCAS No.: 1407966-77-1PF-06465469 (Standard) is the analytical standard of PF-06465469 (HY-108691). This product is intended for research and analytical applications. PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma.
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CXCR7 modulator 1 (Standard)
0 ImagesCat. No.: HY-107987RCAS No.: 2231812-31-8CXCR7 modulator 1 (Standard) is the analytical standard of CXCR7 modulator 1 (HY-107987). This product is intended for research and analytical applications. CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.
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CCR5/CXCR3-IN-1
0 ImagesCat. No.: HY-164630CAS No.: 680203-04-7
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AMD 3465 hexahydrobromide (Standard)
0 ImagesCat. No.: HY-15971RCAS No.: 185991-07-5Synonyms: GENZ-644494 hexahydrobromide (Standard)AMD 3465 (hexahydrobromide) (Standard) is the analytical standard of AMD 3465 (hexahydrobromide). This product is intended for research and analytical applications. AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) 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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Reparixin (Standard)
0 ImagesSynonyms: Repertaxin (Standard); DF 1681Y (Standard)
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MSX-130 (Standard)
0 ImagesCat. No.: HY-103010RCAS No.: 4051-59-6
