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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Olaptesed pegol
0 ImagesCat. No.: HY-160041CAS No.: 1390628-22-4Synonyms: NOX-A12Olaptesed pegol (NOX-A12) is a L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment. Olaptesed pegol can enhances the infiltration of human primary T cells and NK cells and inhibit tumor growth companied with anti-PD-1 antibody. Olaptesed pegol can be used for researches of colon cancer and lymphocytic leukemia.
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UNBS5162
0 ImagesUNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
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LIH383 TFA
0 ImagesCat. No.: HY-P10333APurity: 98.70%LIH383 TFA is an agonist of ACKR3 (CXCR7) (EC50=0.61 nM). LIH383 TFA efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.
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BVT173187
0 ImagesBVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitory activity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.
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CXCL-CXCR1/2-IN-1
0 ImagesCXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects.
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Anti-CXCR3/GPR9/CD183 Antibody
0 ImagesCat. No.: HY-P990394Purity: 98.45%Anti-CXCR3/GPR9/CD183 Antibody is a human-derived antibody expressed in CHO, targeting CXCR3/GPR9/CD183. The Anti-CXCR3/GPR9/CD183 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For the isotype control of Anti-CXCR3/GPR9/CD183 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
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Vimnerixin
0 ImagesSynonyms: AZD4721; RIST4721Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease.
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CXCR2 antagonist 2
0 ImagesCXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunoresearch with an IC50 value of 95 nM.
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Anti-CXCL8/IL-8 Antibody
0 ImagesCat. No.: HY-P990392Purity: 99.51%Anti-CXCL8/IL-8 Antibody is a human antibody expressed in CHO cells that targets CXCL8/IL-8. The Anti-CXCL8/IL-8 Antibody is composed of a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-CXCL8/IL-8 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
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DV1 TFA
0 ImagesCat. No.: HY-P10427APurity: 98.53%DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases.
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Anti-Mouse/Human CXCL12 Antibody (K15C)
0 ImagesCat. No.: HY-P991795Purity: 99.57%Anti-Mouse/Human CXCL12 Antibody (K15C) is an antibody targeting SDF-1/CXCL12. Anti-Mouse/Human CXCL12 Antibody (K15C) blocks the biological activity of SDF-1 secreted by cancer-associated fibroblasts. Anti-Mouse/Human CXCL12 Antibody (K15C) inhibits tumor growth, reduces tumor microvessel density, and decreases the proportion of Sca1+CD31+ endothelial progenitor cells in tumors. Anti-Mouse/Human CXCL12 Antibody (K15C) can be used for research on aggressive human breast cancer. The recommended isotype control is Mouse IgG2a kappa, Isotype Control (HY-P99978).
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pCXCL8-1aa
0 ImagesCat. No.: HY-P10552Purity: 99.07%pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis.
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NI-0801
0 ImagesCat. No.: HY-P990639Purity: 99.19%
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PD-1/PD-L1-IN-63
0 ImagesPD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma.
