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
-
CXCR Related Products (173)
Related Products (173)
-
Olaptesed pegol sodium scrambled negative control
0 ImagesCat. No.: HY-160041BOlaptesed pegol sodium scrambled negative control is the sequence scrambled negative control of Olaptesed pegol sodium.
-
HF51116
0 ImagesCat. No.: HY-144347CAS No.: 2177311-29-2HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis.
-
Plerixafor-d4
0 ImagesCat. No.: HY-10046SCAS No.: 1246819-87-3Plerixafor-d4 is the deuterium labeled Plerixafor. 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.
-
Elubrixin hydrochloride
0 ImagesCat. No.: HY-18263CAS No.: 688763-65-7Synonyms: SB-656933 hydrochlorideElubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.
-
Anti-CXC-ELR Antibody
0 ImagesCat. No.: HY-P990389Anti-CXC-ELR Antibody is a human-derived antibody expressed in CHO, targeting CXC-ELR. Anti-CXC-ELR Antibody is equipped with huIgG4SP type heavy chain and huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-CXC-ELR Antibody can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
-
PD-L1-IN-12
0 ImagesCat. No.: HY-184989PD-L1-IN-12 is an orally active and potent selenium-containing small-molecule PD-L1 inhibitor (KD = 9.06 nM). PD-L1-IN-12 can mediate the internalization of PD-L1 and strongly block hPD-1 and hPD-L1 interaction (IC50 = 5.2 nM). PD-L1-IN-12 can be used in colorectal cancer immunology research.
-
Mz438
0 ImagesCat. No.: HY-155698CAS No.: 3033041-20-9
-
Corydalmine hydrochloride
0 ImagesCat. No.: HY-N2573ACAS No.: 2428393-60-4Synonyms: L-Corydalmine hydrochloride; TLZ-16-CLCorydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi. Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity. Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway.
-
TJX7
0 ImagesCat. No.: HY-P992476TJX7 is a recombinant antibody targeting CXCL13/BCA-1/BLC.
-
AMD 3329 octahydrobromide
0 ImagesCat. No.: HY-164682CAS No.: 170861-77-5AMD 3329 octahydrobromide is a potent and selective anti-HIV-1 and HIV-2 compound with activity to inhibit viral replication. AMD 3329 blocks viral invasion by binding to the chemokine receptor CXCR4. AMD 3329 exhibits EC50 values as low as 0.8 and 1.6 nM when inhibiting HIV-1 and HIV-2 replication, showing better antiviral efficacy than AMD3100. AMD 3329 significantly inhibits the binding of specific CXCR4 monoclonal antibodies and the Ca(2+) flux induced by SDF-1alpha. AMD 3329 is also able to effectively interfere with virus-induced syncytium formation, with an EC50 value of 12 nM.
-
VUF5834
0 ImagesCat. No.: HY-113730CAS No.: 860002-95-5VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
-
cGAS-IN-9
0 ImagesCat. No.: HY-147129CAS No.: 2369750-66-1cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC50 values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC50 of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases.
-
Peptide E5
0 ImagesCat. No.: HY-P11728CAS No.: 1643580-44-2Peptide E5 is an antagonist targeting the CXCR4/CXCL12 axis. Peptide E5 blocks the CXCR4/CXCL12 axis, downregulates CXCR4 expression, and inhibits the phosphorylation of downstream Akt and Erk. Peptide E5 induces apoptosis, suppresses migration and adhesion of breast cancer cells. Peptide E5 inhibits CXCL12-mediated endothelial progenitor cell recruitment, thereby suppressing tumor angiogenesis. Peptide E5 is applicable to relevant research on breast cancer.
-
CXCR4-IN-1
0 ImagesCat. No.: HY-153464CAS No.: 2304750-48-7CXCR4-IN-1 (Example C5) is a CXCR4 inhibitor (IC50: 20 nM). CXCR4-IN-1 can be used for research of cancer, HIV, diabetic retinopathy, inflammation, etc.
