CXCR4 Antibody
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Description
Structure and Target Specificity of CXCR4 Antibodies
CXCR4 antibodies recognize distinct epitopes on the receptor, which spans seven transmembrane domains and contains extracellular, intracellular, and transmembrane regions. Key structural features include:
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The 2B11 clone binds extracellular loops critical for HIV gp120 interaction, enabling viral entry blockade .
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Isoform-specific antibodies like NBP1-77067 selectively detect human isoform b (352 amino acids, 39.7 kDa) but not isoforms a, c, or d .
Mechanisms of Action
CXCR4 antibodies exhibit diverse functional effects depending on their binding sites:
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HIV Inhibition: 2B11 blocks X4-tropic HIV-1/2 entry by interfering with gp120-CD4-CXCR4 complex formation .
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CXCL12 Signaling Disruption: MDX-1338 (BMS-936564) inhibits CXCL12-induced calcium flux (EC50 = 2 nM) and migration in leukemia cells .
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Apoptosis Induction: MDX-1338 triggers caspase-dependent apoptosis in CXCR4+ tumors, independent of complement or effector cells .
Therapeutic Applications in Oncology
Clinical studies highlight CXCR4 antibodies’ efficacy in hematopoietic and solid tumors:
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MDX-1338 showed monotherapy activity in AML and synergized with chemotherapy in preclinical trials .
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Tumors with high CXCR4 expression (e.g., SUM149 breast cancer) respond better to antibody therapy, underscoring the need for biomarker-driven patient selection .
Diagnostic and Imaging Utility
Radiolabeled CXCR4 antibodies enable non-invasive tumor profiling:
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89Zr-CXCR4-mAb: A zirconium-89-conjugated MDX-1338 variant detected CXCR4+ metastases in NSCLC models with high sensitivity .
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Correlation with Therapy: PET imaging with 89Zr-CXCR4-mAb predicted therapeutic response in TNBC and NSCLC, supporting its use for treatment stratification .
Research Applications
CXCR4 antibodies are widely used in experimental settings:
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Flow Cytometry: NBP1-77067 distinguishes CXCR4+ wild-type astrocytes from knockout cells .
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Immunohistochemistry: ACR-014 localizes CXCR4 in human spleen and vascular smooth muscle cells .
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Western Blot: Isoform-specific antibodies resolve CXCR4 variants (40–48 kDa) in lysates .
Challenges and Future Directions
While CXCR4 antibodies show promise, limitations include:
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Isoform Complexity: Few antibodies distinguish between splice variants (e.g., isoform b vs. d) .
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Solid Tumor Penetration: Large antibody molecules may face bioavailability challenges in dense tumors .
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Ongoing trials are exploring combination therapies (e.g., CXCR4 inhibitors + chemotherapy) to overcome resistance .
Product Specs
Buffer
PBS with 0.1% Sodium Azide, 50% Glycerol, pH 7.3. Store at -20°C. Avoid freeze/thaw cycles.
Lead Time
Typically, we can ship your order within 1-3 business days of receiving it. Delivery times may vary depending on the purchasing method and location. Please contact your local distributor for specific delivery time estimates.
Synonyms
CXCR4; C-X-C chemokine receptor type 4; CXC-R4; CXCR-4; FB22; Fusin; HM89; LCR1; Leukocyte-derived seven transmembrane domain receptor; LESTR; Lipopolysaccharide-associated protein 3; LAP-3; LPS-associated protein 3; NPYRL; Stromal cell-derived factor 1 receptor; SDF-1 receptor; CD antigen CD184
Target Names
Uniprot No.
Target Background
Function
CXCR4 (CXC chemokine receptor 4) acts as a receptor for the C-X-C chemokine CXCL12/SDF-1, triggering signal transduction by increasing intracellular calcium ion levels and enhancing MAPK1/MAPK3 activation. It is involved in the AKT signaling cascade and plays a crucial role in regulating cell migration, as seen during wound healing. CXCR4 also functions as a receptor for extracellular ubiquitin, leading to elevated intracellular calcium ions and reduced cellular cAMP levels. It binds bacterial lipopolysaccharide (LPS) and mediates LPS-induced inflammatory responses, including TNF secretion by monocytes. CXCR4 is involved in hematopoiesis and cardiac ventricular septum formation. Furthermore, it plays a critical role in the vascularization of the gastrointestinal tract, likely by regulating vascular branching and/or remodeling processes in endothelial cells. CXCR4 is also implicated in cerebellar development. Within the CNS, it may mediate hippocampal-neuron survival.
In the context of microbial infection, CXCR4 acts as a coreceptor (with CD4 being the primary receptor) for human immunodeficiency virus-1/HIV-1 X4 isolates and as a primary receptor for some HIV-2 isolates. It facilitates Env-mediated fusion of the virus.
Gene References Into Functions
- Functional analysis in human breast cancer cells revealed that LL-37 induced the internalization of CXCR4 by interacting with Glu268, a residue on CXCR4, independent of the binding pocket (Asp171, Asp262, and Glu288) for the CXCR4 inhibitor AMD3100. This suggests that LL-37 acts as a distinct agonist of CXCR4. PMID: 30251699
- Research findings indicate that the S18-2 protein induces epithelial to mesenchymal cell transition via the TWIST2/E-cadherin signaling pathway, ultimately leading to CXCR4-mediated migration of prostate cancer cells. PMID: 29396484
- A study identified a variant near the chemokine receptor CXCR4 that was associated with an increased risk for progressive supranuclear palsy and Parkinson's disease. Moreover, in a mouse model of tauopathy, the expression of CXCR4 and functionally associated genes was significantly altered in brain regions known to accumulate neurofibrillary tangles. PMID: 29636460
- The expression of CXCR4 and mTOR was found to be negatively correlated with remission in patients with cancer. Kaplan-Meier analysis indicated a significant decrease in progression-free survival (PFS) and overall survival (OS) in patients exhibiting positive CXCR4 and mTOR expression. PMID: 28952842
- Evidence suggests that the CXCL12-CXCR4 axis promotes migration, invasion, and epithelial-mesenchymal transition (EMT) processes in B-CPAP cells, at least partially, by activating the NF-kappaB signaling pathway. PMID: 29316404
- Results demonstrate that non-oxidizable HMGB1 induces sustained cardiac fibroblasts migration despite the redox state of the environment, by altering the CXCL12/CXCR4 axis. This effect influences proper cardiac remodeling following an infarction. PMID: 28716707
- CXCR4 is highly abundant in the zona glomerulosa and in aldosterone-producing adenomas, suggesting a significant role in adrenocortical physiology and representing a potential target for molecular imaging of aldosterone-producing tissue. PMID: 29279316
- High CXCR4 expression is associated with bladder cancer progression. PMID: 30015971
- Overexpression of CXCR4 increased soluble vascular cell adhesion molecule 1 (sVCAM1). The sVCAM1 secreted from CXCR4-overexpressing non-small cell lung carcinoma cells recruited and arrested additional osteoclast progenitors, thereby promoting osteoclastogenesis. PMID: 30355915
- MiR-125b functions as an important downstream mediator upon activation of the CXCL12/CXCR4 axis. PMID: 28176874
- Research suggests that CXCL12 and its receptor CXCR4 are crucial in maintaining homeostasis, particularly during hematopoiesis. Ongoing clinical trials, especially in hematological tumors, are investigating whether adding CXCR4 inhibitors to impair tumor dissemination will enhance the effectiveness of existing anti-cancer treatments (CXCL12 = C-X-C motif chemokine ligand 12; CXCR4 = C-X-C motif chemokine receptor-4). [REVIEW] PMID: 29288743
- Hypoxia-induced expression of CXCR4 promoted trophoblast cell migration and invasion via activation of HIF1alpha, a crucial process during placentation. PMID: 29786753
- CXCR4 expression was up-regulated in NSCLC cell lines. Inhibiting CXCR4 may reduce epithelial-mesenchymal transition (EMT), invasion, and migration of NSCLC cells. PMID: 29972256
- Results suggest that BCP-ALL cells create a leukemic niche that attracts leukemic cells in a CXCR4/CXCL12-independent manner. PMID: 28619846
- Serum CXCR4 and CXCL12 levels increase significantly in septic neonates and serve as valuable markers for the diagnosis of neonatal sepsis. These serum concentrations represent promising novel biomarkers for this condition. PMID: 28562124
- A study provided an atomistic-level description of the activation dynamics of the C-X-C chemokine receptor type 4 (CXCR4), a class A GPCR and a significant drug target. PMID: 30238101
- CXCL12 and CXCR4 polymorphisms may be risk factors for hepatocellular carcinoma (HCC) and may serve as potential HCC markers. PMID: 29741398
- Research findings suggest that CXCR4 is a predictor of poor prognosis and may serve as a biomarker for the mesenchymal subtype in patients with Glioblastoma multiforme (GBM). Additionally, CXCR4 mediated the mitogen-activated protein kinase signaling pathway, specifically identified in patients with mesenchymal GBM. PMID: 29767255
- The stromal cell-derived factor-1/C-X-C chemokine receptor type 4 (SDF-1/CXCR4) axis induces human dental pulp stem cell migration through FAK/PI3K/Akt and GSK3beta/beta-catenin pathways. PMID: 28067275
- EGFR over-expression and mutations lead to alterations in the biological characteristics of human lung adenocarcinoma cells through the CXCR4/CXCL12 signaling pathway. PMID: 30037369
- BACH1 may inhibit the progression of colorectal cancer through the BACH1/CXCR4 pathway. PMID: 29481800
- High CXCR4 expression is associated with differential expression patterns in adenocarcinoma and squamous cell carcinoma of the lung relative to small cell lung cancer. PMID: 30076481
- No significant associations were found between mean plasma levels of either CXCL12 or CXCR4 and age, gender, tumor site, tumor size, lymph-node involvement, or tumor stage. PMID: 29693336
- The present study aimed to assess whether fibrosis markers, estrogen receptor (ER)alpha, and the stromal derived factor (SDF)1/CXC chemokine receptor type 4 (CXCR4) axis are abnormally expressed in the endometrium of patients with Intrauterine adhesions. PMID: 29568895
- Daily oral administration of AMD070 significantly inhibited the lung metastasis of B88SDF1 cells in nude mice. These findings suggest that AMD070 could be a potentially useful, novel, orally bioavailable inhibitor of oral cancer metastasis. PMID: 29749473
- Research demonstrated that JWA suppressed the migration/invasion of breast carcinoma cells by downregulating CXCR4 expression. This suggests that JWA may have prognostic and therapeutic potential in patients with breast cancer. PMID: 29658570
- Research suggests that SDF1 (e.g., presented on proteoglycans) can rapidly activate integrins in an allosteric manner by binding to site 2 in the absence of CXCR4. This allosteric integrin activation by SDF1 represents a novel target for drug discovery. PMID: 29301984
- High CXCR4 expression is associated with lymph node metastasis in colorectal cancer. PMID: 29719205
- This effect can be suppressed by miR-613 through direct downregulation of CXCR4. PMID: 29845707
- These results suggest a key role for the CXCR4-CXCL12 chemokine axis in breast cancer progression and highlight its prognostic importance for breast cancer survival. PMID: 29516917
- CXCR4 can induce PI3Kdelta inhibitor resistance in ABC DLBCL. PMID: 29472546
- Research demonstrated greater expression of pRET and CXCR4 in cisplatin-resistant neuroblastomas (NBs). Vandetanib significantly inhibited SHSY5YR cell proliferation, colony formation, and invasion, while downregulating pRET and CXCR4 expression. PMID: 29436676
- Disruption of the CXCR4/CXCL12 axis by the CXCR4 antagonist AMD3100 blocked the contribution of both cancer and stromal cells to the metastatic cascade in the liver. PMID: 29436696
- LncRNA PRNCR1 up-regulates CXCR4 through targeting miR-211-5p, which affects osteogenic differentiation, contributing to osteolysis after hip replacement. PMID: 29775758
- Results demonstrated that miR-1246 inhibited cell invasion and EMT process by targeting CXCR4 and blocking JAK/STAT and PI3K/AKT signal pathways in lung cancer cells. PMID: 29171984
- High CXCR4 expression is associated with hepatocellular and cholangiocellular carcinomas in tumor capillaries. PMID: 29282035
- Each of the CXCR4-derived peptides exhibited high affinity for GroEL with a binding stoichiometry near seven. These peptides interact with the paired alpha helices in the apical domain of the chaperonin. Each of the two chaperonin rings is capable of accommodating all seven CXCR4 peptides bound to GroEL under saturation conditions. ATP alone or combined with GroES promoted the peptide release from... PMID: 29627450
- Down-regulation of CXCR4 significantly reduced cell proliferation while remarkably increasing cell apoptosis and apoptotic protein expression levels in osteosarcoma cells. PMID: 29734183
- Quercetin suppressed breast cancer stem cell proliferation, self-renewal, and invasiveness. It also lowered the expression levels of proteins associated with tumorigenesis and cancer progression, such as aldehyde dehydrogenase 1A1, C-X-C chemokine receptor type 4, mucin 1, and epithelial cell adhesion molecules. PMID: 29353288
- Icaritin enhances mesenchymal stem cell (MSC) proliferation, chemotaxis to stromal cell-derived factor-1, and osteogenic differentiation through STAT-3 activation, leading to an up-regulation in CXCR4 expression and activity. Phosphorylated STAT-3 binds to the CXCR4 promoter, upregulating its expression. PMID: 29679717
- CXCL11 did not significantly alter the (13)C-(1)H-HSQC spectrum of CXCR4. Our findings suggest that ubiquitin acts as a biased agonist of CXCR4. PMID: 28455789
- High CXCR4 expression may define a specific subtype of sporadic malignant peripheral nerve sheath tumor with a favorable prognosis. PMID: 29020982
- Data supports the importance of SDF-1 and CXCR4 expression for loco-regional control and overall survival in head and neck squamous cell carcinoma (HNSCC) after primary radiochemotherapy. PMID: 29061496
- The presence of SST5, CXCR4, and ETA on tumor cells and SST3, CXCR4, and ETA on microvessels gradually increased from grade II to grade IV tumors. PMID: 29696364
- These data revealed that CXCR4 is a novel hepatocellular carcinoma (HCC) vascular marker for vessel sprouting. It could serve as a potential therapeutic target and a predictive factor for sorafenib treatment in patients with HCC. PMID: 28223275
- Hetero-oligomerization of the a1B/D-adrenergic receptor with the chemokine (C-X-C motif) receptor 4: atypical chemokine receptor 3 heteromeric complex is required for a1B/Dadrenergic receptor function. PMID: 28862946
- CXCR4+ cells increased in response to DOXO, primarily in human cardiac mesenchymal progenitor cells (CmPC), a subpopulation with regenerative potential. PMID: 28837147
- This work demonstrates distinct roles for the SDF-1/CXCR4 or CXCR7 network in human induced pluripotent stem cell-derived ventricular cardiomyocyte specification, maturation, and function. PMID: 28711757
- Implantation of IGF1R(+) human dental pulp mesenchymal stem cells exerted enhanced neuroplasticity by integrating inputs from both CXCR4 and IGF1R signaling pathways. PMID: 27586516
- CXCR4 was overexpressed on systemic lupus erythematosus B cells, positively correlating with disease activity and kidney involvement. PMID: 27665947
Database Links
Involvement In Disease
WHIM syndrome (WHIMS)
Protein Families
G-protein coupled receptor 1 family
Subcellular Location
Cell membrane; Multi-pass membrane protein. Cell junction. Early endosome. Late endosome. Lysosome. Note=In unstimulated cells, diffuse pattern on plasma membrane. On agonist stimulation, colocalizes with ITCH at the plasma membrane where it becomes ubiquitinated. In the presence of antigen, distributes to the immunological synapse forming at the T-cell-APC contact area, where it localizes at the peripheral and distal supramolecular activation cluster (SMAC).
Tissue Specificity
Expressed in numerous tissues, such as peripheral blood leukocytes, spleen, thymus, spinal cord, heart, placenta, lung, liver, skeletal muscle, kidney, pancreas, cerebellum, cerebral cortex and medulla (in microglia as well as in astrocytes), brain microv
Customer Reviews
,
B.A
By Anonymous
★★★★★
Applications : Immunohistochemistry (IHC)
Sample type: cell
Review: Representative photomicrographs for immunohistochemical staining of CXCR4. Invasive ductal carcinoma showing moderate [A] and strong [B] cytoplasmic and membranous staining of CXCR4. Brown color indicates positive staining. Negative, weak, moderate and strong staining = 0, 1, 2 and 3, respectively. Magnification: ×400, scale bar: 20 μm.
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