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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Baohuoside I (Standard)
0 ImagesCat. No.: HY-N0011RCAS No.: 113558-15-9Synonyms: Icariin-II (Standard); Icariside-II (Standard)Baohuoside I (Standard) is the analytical standard of Baohuoside I. This product is intended for research and analytical applications. Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
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TRK-530 sodium
0 ImagesCat. No.: HY-19295CAS No.: 151425-92-2TRK-530 sodium is an orally active bisphosphonate. TRK-530 sodium inhibits CINC-1. TRK-530 sodium inhibits dental calculus formation. TRK-530 sodium also inhibits paw edema, joint destruction and osteomyelitis.
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CXCR4-antagonist-12
0 ImagesCat. No.: HY-182908CAS No.: 2892569-27-4
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LIH383
0 ImagesCat. No.: HY-P10333CAS No.: 2866266-58-0LIH383 is an agonist of ACKR3 (CXCR7) (EC50=0.61 nM). LIH383 efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.
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vMIP-II (1-21)
0 ImagesCat. No.: HY-P4109CAS No.: 265650-93-9Synonyms: NT21MP; V1 peptide
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Anti-CXCR3 Antibody (5H7)
0 ImagesCat. No.: HY-P992013
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HBP08
0 ImagesCat. No.: HY-P10321CAS No.: 2490442-13-0HBP08 is a selective inhibitor of CXCL12/HMGB1 interaction. HBP08 has a high affinity for HMGB1 (Kd=0.8 μM). HBP08 inhibits CXCL12-mediated cell migration.
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(±)-AMG 487
0 ImagesCat. No.: HY-15319ACAS No.: 947536-03-0(±)-AMG 487 is a racemate of AMG 487. 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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Catenarin
0 ImagesCatenarin, an anthraquinone compound, inhibits CCR5- and CXCR4-mediated chemotaxis. Catenarin reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), and calcium mobilization. Catenarin shows anti-inflammatory effect and suppresses leukocyte migration in the diabetes. Catenarin exhibits significant inhibitory effects against Gram-positive bacteria. Catenarin prevents type 1 diabetes (T1D) in nonobese diabetic mice[1][2].
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CX4338
0 ImagesCat. No.: HY-119234CAS No.: 41609-06-7CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis.
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Peptide 78
0 ImagesPeptide 78, a chemotactic cytokine, a 78 amino acid protein member of the IL-8 or C-X-C chemokine supergene family. ENA-78 plays an important role in the elicitation of predominantly neutrophils (PMNs) into the joints of rheumatoid arthritis (RA).
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AMD-3329
0 ImagesCat. No.: HY-167945CAS No.: 170861-87-7AMD-3329 is a potent and selective anti-HIV-1 and HIV-2 agent, exhibiting activity by inhibiting virus replication through binding to the chemokine receptor CXCR4, which serves as a co-receptor for the entry of X4 viruses.
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TN14003
0 ImagesCat. No.: HY-131374CAS No.: 368874-31-1TN14003 is a CXCR4 inhibitor. TN14003 has antitumor activity.
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Anti-CXCR2 Antibody
0 ImagesCat. No.: HY-P992036
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Hexaprofen
0 ImagesCat. No.: HY-106463CAS No.: 24645-20-3Hexaprofen is a 2-arylpropionic acid derivative. Hexaprofen inhibits CXCL8-induced chemotaxis, while no activity is detected against CXCL1-induced chemotaxis.
