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 (174)
Related Products (174)
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MSX-130 (Standard)
0 ImagesCat. No.: HY-103010RCAS No.: 4051-59-6
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BI-1607
0 ImagesCat. No.: HY-P991582BI-1607 is a humanized monoclonal antibody targeting FcγRIIB/CD32b. BI-1607 selectively blocks inhibitory FcγRIIB signaling, abrogates its inhibitory function, redirects tumor cell-bound antibodies to activating FcγRs, and its modified Fc region prevents the binding of its own Fc segment to FcγRs. BI-1607 reduces αPD-1 trogocytosis, enhances the effector functions of anti-tumor antibodies (including ADCP and ADCC, promotes intratumoral regulatory T cell (Treg) depletion, myeloid cell reprogramming, induction of interferon-γ (IFN-γ) and CXCL10, and increases the number of activated effector CD8+ T cells. BI-1607 can be used in research related to colorectal cancer, HER2-positive advanced solid tumors, HER2-positive locally advanced or metastatic breast cancer, and HER2-positive metastatic gastric cancer.
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Navarixin (Standard)
0 ImagesCat. No.: HY-10198RCAS No.: 473727-83-2Synonyms: SCH 527123 (Standard); MK-7123 (Standard)Navarixin (Standard) is the analytical standard of Navarixin (HY-10198). This product is intended for research and analytical applications. Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
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(Rac)-SCH 563705 (Standard)
0 ImagesCat. No.: HY-10011BRCAS No.: 2701435-64-3(Rac)-SCH 563705 (Standard) is the analytical standard of (Rac)-SCH 563705 (HY-10011B). This product is intended for research and analytical applications. (Rac)-SCH 563705 is a racemic mixture of SCH 563705 (HY-10011). SCH 563705 (compound 16) is a potent and orally active CXCR2 and CXCR1 antagonist with IC50 values of 1.3 nM and 7.3 nM and Ki values of 1 nM and 3 nM, respectively.
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Elubrixin tosylate (Standard)
0 ImagesCat. No.: HY-18263CRCAS No.: 960495-43-6Synonyms: SB-656933 tosylate (Standard)Elubrixin (tosylate) (Standard) is the analytical standard of Elubrixin (tosylate). This product is intended for research and analytical applications. 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.
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SCH 563705 (Standard)
0 ImagesCat. No.: HY-10011RCAS No.: 473728-58-4SCH 563705 (Standard) is the analytical standard of SCH 563705 (HY-10011). This product is intended for research and analytical applications. 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.
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Olopatadine-d3 (hydrochloride)
0 ImagesCat. No.: HY-B0426ASCAS No.: 1331635-21-2Olopatadine-d3 hydrochloride (ALO4943A-d3) is the deuterium labeled Olopatadine hydrochloride. Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4+ and CD8+ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis.
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Plerixafor (Standard)
0 ImagesSynonyms: AMD 3100 (Standard); JM3100 (Standard); SID791 (Standard)Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
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Anti-Mouse ACKR4 Antibody (A4Mab-3)
0 ImagesCat. No.: HY-P991785Anti-Mouse ACKR4 Antibody (A4Mab-3) reacts with atypical chemokine receptor 4 (ACKR4). ACKR4 is a seven-transmembrane domain-containing protein that belongs to the atypical chemokine receptors (ACKRs) family. Recommend Isotype Controls: Rat IgG2b kappa, Isotype Control (HY-P990682).
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IT1t dihydrochloride (Standard)
0 ImagesCat. No.: HY-101458ARCAS No.: 1092776-63-0IT1t (dihydrochloride) (Standard) is the analytical standard of IT1t (dihydrochloride) (HY-101458A). This product is intended for research and analytical applications. IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
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AMG 487 (Standard)
0 ImagesCat. No.: HY-15319RCAS No.: 473719-41-4AMG 487 (Standard) is the analytical standard of AMG 487 (HY-15319). This product is intended for research and analytical applications. AMG 487 is an orally active and selective antagonist of CXC chemoKine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
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PS372424 hydrochloride (Standard)
0 ImagesCat. No.: HY-111149ARCAS No.: 1596362-29-6PS372424 hydrochloride (Standard) is the analytical standard of PS372424 (hydrochloride) (HY-111149A). This product is intended for research and analytical applications. PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation.
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NUCC-390 dihydrochloride (Standard)
0 ImagesCat. No.: HY-111793ARCAS No.: 2749281-71-6NUCC-390 dihydrochloride (Standard) is the analytical standard of NUCC-390 (dihydrochloride) (HY-111793A). This product is intended for research and analytical applications. NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.
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Anti-CD185/CXCR5 Antibody
0 ImagesCat. No.: HY-P991227Synonyms: BAY-924 antibodyAnti-CD185/CXCR5 Antibody is an antibody inhibitor, targeting to human CD185/CXCR5.
