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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. -
CXCR3 Antagonist
Hypoglaucin A is a CXCR3 antagonist with an IC50 value of 0.47 μM, exhibiting significant inhibitory effects on CXCR3-mediated signaling pathways. This compound is particularly relevant for research into inflammatory processes, as CXCR3 is implicated in various immune responses. Hypoglaucin A can be utilized to investigate the role of CXCR3 in inflammation-related studies and potential therapeutic applications. -
CXCR4 Antagonist
CXCR4 antagonist 8 is a selective antagonist of the CXCR4 receptor, demonstrating an IC50 of 57 nM. It effectively inhibits CXCL12-induced increases in cytosolic calcium with an IC50 value of 0.24 nM. This compound is valuable for investigating CXCL12/CXCR4-mediated cell migration and cellular signaling pathways related to various biological processes, including cancer metastasis and immune cell trafficking. -
CXCR1/CXCR2 Antagonist
SX-576 is a potent antagonist of CXCR1 and CXCR2, exhibiting IC50 values of 31 nM and 21 nM, respectively. This compound effectively inhibits neutrophil infiltration in rat models of pulmonary inflammation, making it a valuable tool for research into inflammatory diseases. SX-576 is suitable for investigations focused on the role of these chemokine receptors in pulmonary inflammation and related pathologies. -
Stable Isotope
Nicotinamide N-oxide-d4 is a deuterium-labeled derivative of Nicotinamide N-oxide, which serves as a stable isotope for analytical studies. As a notable in vivo metabolite of nicotinamide, Nicotinamide N-oxide exhibits potent and selective antagonistic activity against the CXCR2 receptor. This compound is valuable for research applications involving receptor signaling, metabolic pathways, and the study of inflammatory responses. -
CXCR Antagonist
VUF10132 is a non-peptide antagonist targeting the CXCR3 receptor, demonstrating significant anti-inflammatory activity. It effectively inhibits conditions such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has a high affinity for the human CXCR3 receptor, with a slightly lower affinity for the murine counterpart, and also exhibits inverse agonist properties, making it a valuable tool for studying CXCR3-related signaling in various inflammatory diseases. -
CXCR3 Activator
VUF11418 is an activator of the chemokine receptor CXCR3. This compound plays a significant role in modulating inflammatory responses and is valuable for studying inflammation-related pathways. VUF11418 is particularly useful in research applications focusing on immune responses and related therapeutic strategies. -
CXCL12 Inhibitor
4-Amino-D-phenylalanine is a potent CXCL12 inhibitor that targets the CXCR4 receptor. With an IC50 value of 0.1 μM, it effectively inhibits the binding of CXCL12 to its receptor. This compound is valuable for research applications focused on understanding CXCR4-related pathways and their implications in cancer, inflammation, and various other diseases. -
CXCR2 Antagonist
CXCR2 antagonist 3 is a potent inhibitor of CXC chemokine receptor 2 (CXCR2), exhibiting double-digit nanomolar potency. It effectively reduces neutrophil and myeloid-derived suppressor cell (MDSC) infiltration while promoting the infiltration of CD3+ T lymphocytes in Pan02 tumor tissues. This antagonist is valuable for research applications focusing on inflammation and tumor microenvironment remodeling. -
hKOR Activator
BAM-12P is a pro-Met-enkephalin that functions as a selective activator of the human κ-opioid receptor (hKOR), exhibiting an EC50 value of 101 nM. Additionally, BAM-12P also interacts with the CXCR7 receptor, with an EC50 of 175 nM. This compound is valuable in research applications investigating opiate receptor signaling pathways and the role of endogenous peptides in pain modulation and neurobiology. -
ACKR3 (CXCR7) Agonist
LIH383 is a selective agonist of ACKR3 (CXCR7) with an EC50 of 0.61 nM. This compound effectively promotes the recruitment of β-arrestin to ACKR3, while distinctly lacking the activation of classical G protein signaling pathways. LIH383 is useful for studies investigating the role of ACKR3 in cellular processes and its potential therapeutic applications in various diseases. -
CXCR4 Inhibitor
vMIP-II (1-21) is a selective inhibitor of the chemokine receptor CXCR4. By competing with 125I-SDF-1R for binding sites, vMIP-II (1-21) effectively disrupts CXCR4 signaling, with an IC50 value of 190 nM. This compound is useful for research applications involving the study of chemokine receptors and their role in various biological processes, such as immune response and cancer metastasis. -
CXCR4 Antagonist
BPRCX 714 is an antagonist of the CXCR4 (CXC chemokine receptor type 4), a critical receptor implicated in various cancer metastasis processes. It exhibits potential therapeutic effects by inhibiting CXCR4 signaling, making it valuable for research into hepatocellular carcinoma and other CXCR4-related malignancies. Its application in studies enhances understanding of tumor microenvironment interactions and provides insights into targeted cancer therapies. -
CXCR3 Antagonist
(±)-AMG 487 is a selective antagonist of CXC chemokine receptor 3 (CXCR3), effectively inhibiting the binding of CXCL10 and CXCL11 with IC50 values of 8.0 nM and 8.2 nM, respectively. This compound demonstrates significant potential in studying immune responses and inflammatory processes due to its ability to block CXCR3-mediated signaling. Its oral bioavailability enhances its utility in preclinical and clinical research applications targeting inflammatory diseases and cancer. -
CXCR4 Antagonist
ICT5040 is a small molecule antagonist targeting the chemokine receptor CXCR4, with an IC50 of 3.8 μM. This compound effectively inhibits CXCL12-mediated cell proliferation and migration in glioma cells, specifically U87 cells, and suppresses CXCL12-induced intracellular calcium mobilization. ICT5040 serves as a valuable tool for investigating the role of the CXCR4/CXCL12 axis in cancer research and potential therapeutic applications.

