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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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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NI-0701
0 ImagesCat. No.: HY-P990638Purity: 99.74%NI-0701 is a humanized antibody expressed in CHO cells that targets CCL5/RANTES. NI-0701 has a huIgG2 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for NI-0701 can be referenced as Human IgG2 lambda, Isotype Control (HY-P991206).
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Cyclic MKEY TFA
0 ImagesCat. No.: HY-P1949APurity: 98.47%Cyclic MKEY TFA is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY TFA also protects against stroke-induced brain injury in mice.
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Anti-Mouse CCL5 Antibody (R6G9)
0 ImagesCat. No.: HY-P991753Anti-Mouse CCL5 Antibody (R6G9) is a neutralizing agent that binds to CCL5 to inhibit its chemotactic activity towards CD4+ T cells.Anti-Mouse CCL5 Antibody (R6G9) does not suppress CD4+ T cell migration towards infection-derived liver cells, reduce CD4+ T cell hepatic accumulation, or impair CD4+ T cell migratory capacity.Anti-Mouse CCL5 Antibody (R6G9) serves as a tool to assess CCL5’s role in in vivo target cell killing by LCMV-specific CD8+ effector T cells.Anti-Mouse CCL5 Antibody (R6G9) can be used for the research of malaria infection and lymphocytic choriomeningitis virus infection.
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(±)-NBI-74330
0 Images(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model.
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(R,R)-CXCR2-IN-2
0 Images(R,R)-CXCR2-IN-2 (compound 67), diastereoisomer of CXCR2-IN-2 (compound 68) (HY-120878), is a CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
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DPM-1003
0 ImagesCat. No.: HY-160550CAS No.: 3018836-86-4DPM-1003 is a modulator of protein tyrosine phosphatase 1B (PTP1B) and C-X-C chemokine receptor 4 (CXCR4). DPM-1003 binds to the non-catalytic disordered C-terminal fragment of PTP1B. DPM-1003 inhibits the PI3Kγ-mediated AKT/mTOR signaling pathway downstream of CXCR4. DPM-1003 improves the survival rate of mice in a transfusion-related acute lung injury model, and exerts a lung injury protective effect in preclinical mouse models of acute lung injury and sepsis. DPM-1003 can be used in research related to acute lung injury, acute respiratory distress syndrome, transfusion-related acute lung injury and sepsis.
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CCX-777 formic
0 ImagesCat. No.: HY-123813APurity: 98.01%CCX-777 formic is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 formic induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 formic functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 formic is widely used in cancer-related research.
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PF-06835375
0 ImagesCat. No.: HY-163480CAS No.: 2796997-12-9PF-06835375 is a selective, humanized CXCR5-targeting immunoglobulin G1 antibody. PF-06835375 depletes CXCR5-positive B cells, follicular helper T cells and circulating Tfh-like cells. PF-06835375 is applicable to research related to autoimmune diseases.
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(Rac)-SCH 563705
0 Images(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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Anti-Human/Mouse/Monkey CXCR3 Antibody (9C5)
0 ImagesCat. No.: HY-P992014Purity: 99.33%
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Anti-CXCL12/SDF1a Antibody
0 ImagesCat. No.: HY-P990390Purity: ≥99.0%Anti-CXCL12/SDF1a Antibody is a CHO-expressed human antibody that targets CXCL12/SDF1a. The Anti-CXCL12/SDF1a Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. For the isotype control of Anti-CXCL12/SDF1a Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
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Plerixafor solution
0 ImagesCat. No.: HY-FL10046CAS No.: 110078-46-1Synonyms: AMD 3100 solution; JM3100 solution; SID791 solutionPlerixafor solution is mainly composed of Plerixafor (HY-10046). 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.
