Catalog No.
Product Name
Application
Product Information
Citations
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CXCR2/1 Antagonist
SX-517 is a dual antagonist of CXCR2 and CXCR1, featuring a boronic acid structure. It effectively inhibits CXCL1-induced calcium flux with an IC50 of 38 nM and disrupts CXCL8-induced [(35)S]GTPγS binding, showing an IC50 of 60 nM, while also preventing ERK1/2 phosphorylation. This compound demonstrates significant anti-inflammatory properties in both humanized polymorphonuclear (PMN) cells and murine models, making it a valuable tool for research into inflammation-related pathways. -
Isomer
(Rac)-Reparixin is an isomer of Reparixin and serves as a useful experimental control in research settings. Reparixin functions as a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2, exhibiting inhibitory constants (IC50) of 1 nM and 100 nM, respectively. This compound is valuable for studies focusing on inflammation, cancer biology, and other pathways mediated by chemokine signaling. -
Dual CXCR1/2 Antagonist
Ladarixin sodium is a dual antagonist of CXCR1 and CXCR2, exhibiting an allosteric non-competitive mechanism. This compound demonstrates significant anti-inflammatory activity, making it relevant for research in chronic obstructive pulmonary disease (COPD) and asthma. Its ability to inhibit CXCR1 and CXCR2 pathways positions Ladarixin sodium as a valuable tool for exploring therapeutic strategies in respiratory inflammatory conditions. -
CXCR2 Antagonist
CXCR2-IN-2 is a selective antagonist of the CXCR2 receptor, demonstrating high potency with an IC50 of 5.2 nM in a β-arrestin assay and 1 nM in the CXCR2 Tango assay. This compound exhibits significant selectivity, being approximately 730-fold more selective for CXCR2 over CXCR1 and greater than 1900-fold over other chemokine receptors. Additionally, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood with an IC50 of 0.04 μM, making it a valuable tool for research into inflammatory processes and associated therapeutic applications. -
CXCR Modulator
CXCR7 modulator 2 is a selective modulator of C-X-C Chemokine Receptor Type 7 (CXCR7), exhibiting an affinity with a Ki value of 13 nM. This compound plays a critical role in research applications focusing on chemokine signaling pathways and their involvement in various physiological and pathological processes. It is particularly useful in studies related to cancer metastasis, inflammation, and cardiovascular diseases, making it a valuable tool for understanding CXCR7's biological functions. -
CXCR2 Antagonist
CXCR2 antagonist 8 is a potent and selective antagonist of the CXCR2 receptor, involved in inflammatory responses and immune cell migration. This compound has demonstrated significant activity in models of insulin resistance, making it a valuable tool for investigating metabolic disorders and related signaling pathways. Researchers can utilize CXCR2 antagonist 8 for studies aimed at elucidating the role of CXCR2 in various disease states. -
CXCR4 Receptor Agonist
NUCC-390 is a selective small-molecule agonist of the CXCR4 receptor. This compound induces internalization of CXCR4 receptors, thereby modulating signaling pathways distinct from antagonists. Research indicates that NUCC-390 promotes functional recovery of nerve tissue following neurodegeneration, making it a valuable tool for applications related to neurobiology and regenerative medicine. -
CXCR4 Antagonist
EPI-X4 is a selective antagonist of the C-X-C motif chemokine receptor 4 (CXCR4), exhibiting an IC50 of 8.6 μM. This compound effectively inhibits CXCL12-mediated signaling and reduces chemokine-driven migration and invasion in leukemia cells. Additionally, EPI-X4 demonstrates anti-inflammatory properties in mouse models and displays antiviral activity against CXCR4-tropic HIV, making it a valuable tool for research in cancer, inflammation, and virology. -
CXCR3 Antagonist
ACT-660602 is an orally active antagonist of the chemokine receptor CXCR3, demonstrating an IC50 value of 204 nM. This compound effectively inhibits T-cell migration, making it a valuable tool in the study of immune response. ACT-660602 has shown efficacy in models of acute lung injury and is relevant for research focused on autoimmune diseases and related inflammatory conditions. -
CXCR2 Antagonist
SB-332235 is a potent, orally active nonpeptide antagonist of the chemokine receptor CXCR2, exhibiting an IC50 of 7.7 nM and demonstrating 285-fold selectivity for CXCR2 over CXCR1. This compound has been shown to effectively inhibit both acute and chronic models of arthritis in rabbits. Additionally, SB-332235 reduces the viability of acute myeloid leukemia (AML) cells, indicating its potential utility in cancer research and therapeutic applications for inflammatory diseases. -
CXCR3 Antagonist
CXCR3 antagonist 1 is a selective and non-cytotoxic antagonist of the CXCR3 receptor, exhibiting an IC50 of 0.06 µM. This compound plays a significant role in the research of inflammatory diseases, including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes. Its ability to inhibit CXCR3 activity makes it a valuable tool for elucidating the mechanisms underlying various inflammatory conditions. -
CXCR
BVT173187 is a selective inhibitor of the CXCR target, effectively blocking the activation of the neutrophil formyl peptide receptor FPR1. This compound suppresses FPR1 agonist-induced activation in neutrophils, leading to decreased mobilization of adhesion molecules and reduced superoxide anion production. In addition to its strong effects on FPR1, BVT173187 also influences C5aR and CXCR signaling pathways, making it a valuable tool for research in inflammation and immune response. -
ELR+CXCL-CXCR1/2 Inhibitor
CXCL-CXCR1/2-IN-1 is an orally active inhibitor of the ELR+CXCL-CXCR1/2 signaling pathway, exhibiting an EC50 of 42.7 nM for the CXCR2 receptor. This compound demonstrates significant anticancer and antiangiogenic properties, making it a valuable tool for research into tumor progression and vascularization. Its ability to target these pathways underscores its potential application in cancer biology and therapeutic development. -
CXCR Antagonist
CXCR2 antagonist 2 is a potent antagonist targeting the chemokine receptor CXCR2, with an IC50 value of 95 nM. It exhibits significant biological activity by inhibiting CXCR2-mediated signaling pathways, which are implicated in cancer progression and inflammation. This reagent is particularly valuable for researchers investigating the role of CXCR2 in tumor microenvironments and the development of novel cancer immunotherapies. -
CXCR2 Antagonist
AZD8309 is an orally active CXCR2 antagonist that modulates neutrophil transmigration. This compound is instrumental in studying inflammatory diseases, providing insights into the role of CXCR2 in immune response and potential therapeutic interventions. Researchers can utilize AZD8309 to explore novel treatments aimed at managing conditions characterized by neutrophil-mediated inflammation. -
CXCR2 Antagonist
Vimnerixin is a selective CXCR2 antagonist that actively blocks the acidic CXC chemokine receptor 2, thereby modulating inflammatory responses. This compound demonstrates significant activity in inhibiting CXCR2-mediated signaling pathways, making it a valuable tool for investigating various inflammatory diseases. Research applications include studying the role of CXCR2 in inflammation and potential therapeutic strategies for related conditions. -
CXCR2/CCR7 Antagonist
CCR7 antagonist 1 is a potent dual antagonist of CXCR2 and CCR7, exhibiting an IC50 of 11.02 μM for CXCR2 and 0.43 μM for CCR7. This compound demonstrates significant inhibition of chemokine receptor signaling, making it valuable for studying inflammatory responses and immune system modulation. Its application spans various fields, including cancer research and autoimmune disease studies, where targeting these receptors can provide insights into disease mechanisms and potential therapeutic strategies. -
CXCR4 Antagonist
EMU-116 is a selective antagonist of the CXCR4 receptor. This compound effectively inhibits CXCR4 signaling, which plays a crucial role in tumor growth and metastasis. EMU-116 is relevant for research investigating cancer progression and the implications of CXCR4 in various malignancies. -
CXCR4 Inhibitor
CXCR4-IN-3 is a potent inhibitor of the CXCR4 receptor, demonstrating an IC50 of 3.2 nM. It exhibits significant antichemotactic effects, with an inhibition rate of 79.19±2.33%. This compound also displays anti-inflammatory properties, making it a valuable tool for research into inflammatory bowel disease (IBD) and related inflammatory conditions. -
CXCR3 Agonist
VUF 11222 is a CXCR3 agonist that functions as a non-peptide-like compound, activating the CXCR3 receptor. This reagent is valuable for investigating the role of CXCR3 in inflammatory processes and related immune responses. Its application spans various research areas, including immunology and the study of inflammatory diseases. -
CXCR3 Antagonist
(±)-NBI-74330 is a potent and selective antagonist of the chemokine receptor CXCR3. This compound is effective in alleviating tactile and thermal hypersensitivity and demonstrates the ability to enhance the analgesic effects of morphine. In a rat neuropathic pain model, (±)-NBI-74330 reduces microglial cell activation, promotes astroglial cell activation, and downregulates specific CXCR3 ligands, making it a valuable tool for research in pain modulation and neuroinflammation. -
CXCR2 Antagonist
(R,R)-CXCR2-IN-2 is a selective antagonist of the CXCR2 receptor, exhibiting a robust pIC50 of 9 in the Tango assay and 6.8 in the HWB Gro-α induced CD11b expression assay. This compound demonstrates significant inhibition of CXCR2-mediated signaling pathways, making it a valuable tool for research into inflammatory responses and immune cell migration. Its modulation of CXCR2 activity is pertinent for studies aimed at understanding various disease states, including cancer and chronic inflammatory conditions. -
CXCR4 Inhibitor
Peptide R is a cyclic peptide that functions as a specific antagonist of the CXCR4 receptor. It demonstrates significant efficacy in remodeling tumor stroma, making it a valuable tool for tumor research. Its ability to modulate the tumor microenvironment highlights its potential applications in cancer therapy and investigation into tumor progression mechanisms. -
CXCR7 Antagonist
CCX662 is a CXCR7 antagonist that effectively inhibits the binding of 125I-CXCL12 to the CXCR7 receptor, demonstrating an IC50 value of 9 nM. This compound plays a crucial role in anti-cancer research by modulating the CXCR7 signaling pathway, which is implicated in tumor progression and metastasis. Its ability to disrupt CXCL12/CXCR7 interactions makes it a valuable tool for investigating the role of this pathway in cancer biology. -
Anti-CXCR5 Antibody
PF-06835375 is a humanized IgG1 antibody targeting CXCR5, which is predominantly expressed on B cells, T follicular helper (Tfh) cells, and circulating Tfh-like (cTfh) cells. This antibody is useful for investigating the pathophysiology of systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). Its specificity for CXCR5 makes it a valuable tool in studies focused on immune response and B-cell development in autoimmune diseases. -
SCH 563705 Racemic Mixture
(Rac)-SCH 563705 is a racemic mixture targeting the CXCR1 and CXCR2 receptors, acting as a potent antagonist. With IC50 values of 1.3 nM and 7.3 nM, and Ki values of 1 nM and 3 nM for CXCR2 and CXCR1, respectively, this compound demonstrates significant inhibition of these chemokine receptors. It is primarily utilized in research focused on inflammatory diseases and immune response modulation. -
CXCR4 Antagonist
HF51116 is a potent CXCR4 antagonist that effectively inhibits SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. This compound also demonstrates a capacity to impede HIV-1 infection by targeting the CXCR4 pathway. HF51116 is valuable for research in areas including HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis. -
CXCR2 Receptor Antagonist
AZ10397767 is a selective antagonist of the CXCR2 receptor, exhibiting an IC50 of 1 nM. This compound effectively reduces NF-κB transcriptional activity induced by Oxaliplatin and enhances apoptosis in androgen-independent prostate cancer (AIPC) cells. Additionally, AZ10397767 significantly diminishes neutrophil recruitment to tumors, which may inhibit tumor growth in both in vitro and in vivo models, making it a valuable tool in cancer research. -
Fluorescent Probe
Mz438 is a high-affinity fluorescent ligand targeting the chemokine receptor CXCR2. This small-molecule fluorescent probe is designed to visualize CXCR2 dynamics in live cells, making it a valuable tool for studying cellular signaling and migration in various biological systems. Its selectivity and binding properties facilitate research in inflammation and related diseases, enabling deeper insights into the role of CXCR2 in immune responses. -
CXCR4 Antagonist
Burixafor is a selective antagonist of the CXCR4 receptor that effectively inhibits the binding of CXCL12, with a pIC50 of 7.4. This compound disrupts CXCL12-induced recruitment of Gαᵢ and β-arrestin2, further blocking the Gαᵢ-mediated inhibitory effects on cAMP signaling pathways. Burixafor is instrumental in mobilizing CD34+ hematopoietic stem/progenitor cells from the bone marrow to peripheral blood, making it valuable for research applications in autologous hematopoietic stem cell transplantation. -
CXCR6 Antagonist
CXCR6 antagonist 1 is a selective antagonist of the CXCR6 receptor, which plays a critical role in immune cell trafficking and tumor microenvironment modulation. This compound effectively inhibits CXCR6-mediated signaling pathways, including β-arrestin recruitment and cAMP production induced by Forskolin. Additionally, CXCR6 antagonist 1 demonstrates significant efficacy in reducing tumor growth in a mouse xenograft model of hepatocellular carcinoma. It is a valuable tool for research applications focused on hepatocellular carcinoma and therapeutic strategies targeting CXCR6. -
CXCR Antagonist
VUF5834 is a non-peptide antagonist of the chemokine receptor CXCR3, exhibiting both non-competitive antagonistic and inverse agonistic activities. This compound effectively inhibits the effects of the chemokines CXCL10 and CXCL11 on human CXCR3. Notably, VUF5834 demonstrates a slightly lower affinity for rodent CXCR3 compared to primate CXCR3, making it a useful tool for investigating CXCR3-mediated pathways in various biological research applications. -
peptide
Polyphemusin II-Derived Peptide (T140) is a potent CXCR4 inhibitor that effectively blocks HIV-1 entry into host cells. Its mechanism involves disrupting the interaction between CXCR4 and the HIV-1 envelope glycoprotein, offering a targeted approach to HIV research. Additionally, T140 has been shown to inhibit the binding of the anti-CXCR4 monoclonal antibody (12G5) to its receptor, making it a valuable tool for studying CXCR4-related pathways and potential therapeutic interventions in viral infections. -
CXCR4 Inhibitor
CXCR4-IN-1 is a selective inhibitor of the CXCR4 chemokine receptor, with an IC50 of 20 nM. This compound exhibits potential biological activity in modulating cellular responses associated with cancer progression, HIV infection, diabetic retinopathy, and inflammatory conditions. CXCR4-IN-1 is suitable for use in research applications focused on these disease processes, providing valuable insights into therapeutic targeting of the CXCR4 signaling pathway. -
CXCR4 Modulator
CXCR4 modulator-1 is a selective modulator of the CXCR4 receptor, exhibiting a potent EC50 value of 100 nM. This compound plays a critical role in various biological processes, including inflammation, cancer progression, and HIV pathology. CXCR4 modulator-1 is suitable for research applications focusing on anti-inflammatory mechanisms, anticancer therapies, and HIV treatment studies. -
Mononuclear Cells Chemoattractant
SDF-1α (human) is a potent chemoattractant for mononuclear cells that targets the CXCR4 receptor. This cytokine plays a critical role in various biological processes, including stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis, and ventricular remodeling following myocardial infarction. SDF-1α (human) is primarily utilized in research focused on cardiovascular diseases and regenerative medicine. -
CXCR4 Antagonist
CXCR4 antagonist 5 is a potent antagonist targeting the CXCR4 receptor, exhibiting an IC50 value of 8.8 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium influx with an IC50 of 0.02 nM and blocks CXCR4/CXCL12-mediated chemotaxis. Additionally, CXCR4 antagonist 5 demonstrates favorable physicochemical properties along with a moderate safety profile in vitro, showing minimal inhibition of CYP isozymes and hERG channels. -
CXCR3 Antagonist
(R)-SCH 546738 is a selective antagonist of the CXCR3 receptor, exhibiting non-competitive inhibition with a Ki value of 0.4 nM. This compound demonstrates potent biological activity against CXCR3, making it valuable for research applications targeting inflammatory diseases and immune responses. Its oral bioavailability enhances its utility in in vivo studies, facilitating a deeper understanding of CXCR3-related signaling pathways. -
CXCR4 Antagonist
CXCR4 Antagonist 9 is a potent inhibitor of the CXCR4 receptor, exhibiting an IC50 value of 15 nM. This compound effectively suppresses CXCL12-induced increases in cytosolic calcium levels, with a notable IC50 of 1.3 nM. It is valuable for research applications focused on cell signaling pathways and the modulation of immune responses involving the CXCR4/CXCL12 axis. -
CXCR4 Antagonist
CXCR4 Antagonist 3 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 of 11 nM. This compound, a congener of TIQ15, showcases excellent properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. It is a valuable reagent for research focused on human immunodeficiency virus and related pathologies. -
Biochemical Assay Reagent
SFB-AMD3465 is a derivative of AMD3465, serving as a biochemical assay reagent. This compound functions as a positron emission tomography (PET) tracer for the chemokine receptor CXCR4 when labeled with radioactive fluorine. It is a valuable tool for exploring CXCR4-related signaling pathways and has applications in cancer research and imaging studies. -
CXCR7 Agonist
VUF11207 TFA is a potent agonist of the CXCR7 receptor, exhibiting a pKi of 8.1. This compound effectively induces the recruitment of β-arrestin2, with an EC50 value of 8.8, and facilitates the internalization of CXCR7, demonstrating an EC50 of 7.9. VUF11207 TFA is valuable for research applications focusing on CXCR7 signaling pathways and their implications in various biological processes. -
CXCR2 Inhibitor
NVP CXCR2 20 is a selective inhibitor of the CXCR2 receptor, primarily involved in modulating pain pathways. It exhibits significant analgesic and antinociceptive effects, effectively reducing mechanical and thermal hypersensitivity in rat models of chronic constriction injury (CCI). Additionally, NVP CXCR2 20 diminishes CXCL3-induced hypersensitivity in naive mice and lowers CXCL3 protein levels in the spinal cord and dorsal root ganglia of CCI-exposed rats. This compound is valuable for research into neuropathic pain and chronic obstructive pulmonary disease (COPD). -
CXCR3 Antagonist
ACT-672125 is a potent antagonist of the CXCR3 receptor, exhibiting an IC50 value of 239 nM in human blood. Additionally, it shows hERG activity with an IC50 of 18 μM. This compound is primarily utilized in research investigating autoimmune diseases, providing insights into the modulation of immune responses. -
CXCR4 Antagonist
TIQ-15 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 value of 6 nM for CXCR4-mediated Ca2+ flux. Additionally, it demonstrates inhibition of CYP450 2D6 with an IC50 of 0.32 μM. This compound is valuable for research into CXCR4-related signaling pathways and drug metabolism. -
Inverse CXCR3 Agonist
VUF11211 is an allosteric inverse agonist of the CXCR3 receptor, exhibiting a dissociation constant (Kd) of 0.65 nM. This compound modulates CXCR3 signaling pathways, influencing immune cell migration and activation. VUF11211 is primarily used in research focused on inflammation, autoimmune diseases, and cancer immunotherapy, providing insights into the role of CXCR3 in various pathological conditions. -
Radiolabeled Peptide
Pentixather is a radiolabeled peptide that specifically targets the CXCR4 receptor. By interfering with the CXCR4/CXCL12 signaling axis, Pentixather disrupts the interaction between leukemic cells and the bone marrow microenvironment, thereby promoting the release of leukemic cells from the protective niche and increasing their sensitivity to therapeutics. This compound is valuable for research applications in acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). -
CXCR4 ligand
SDNUM04 is a ligand for the C-X-C chemokine receptor 4 (CXCR4), known for its role in cell migration and metastasis. This compound can be utilized as a tracer in tumor-targeting studies, facilitating research on cancer biology and the mechanisms of tumor progression. Additionally, SDNUM04 may serve as a valuable tool in drug discovery and development focused on CXCR4-related pathways. -
CXCR4 Modulator
CXCR4 modulator-2 is a potent antagonist of the CXCR4 receptor with an IC50 value of 1.25 nM. It demonstrates significant stability in mouse serum, with a half-life of 77.1 minutes, and showcases anti-inflammatory effects in mouse edema models. This compound is valuable for research in inflammation and immune response modulation. -
CXCR4 Antagonist
IS4 is a selective competitive antagonist of the CXCR4 receptor, exhibiting an IC50 of 0.65 nM in THP-1 cells and 38.75 nM in Jurkat cells. It effectively inhibits CXCL12-induced intracellular Ca2+ release and cancer cell migration by binding to CXCR4. Due to its stability in serum and low cytotoxicity, IS4 is valuable for research into the prevention of metastasis in various cancers, including breast cancer, prostate cancer, and leukemia.
