Catalog No.
Product Name
Application
Product Information
Citations
- Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic antagonist of the CXCR4 receptor, with IC50 values below 10 nM. It demonstrates over 1000-fold selectivity for CXCR4 compared to other receptors, including CXCR7. Balixafortide effectively blocks β-arrestin recruitment and calcium flux, and is a strong mobilizer of hematopoietic stem and progenitor cells (HSPCs). It also exhibits anti-cancer activity, making it a promising candidate for oncology and hematology research.
-
CXCR1/CXCR2 antagonist
Ladarixin (DF 2156A free base) is an orally active, allosteric, non-competitive antagonist of the chemokine receptors CXCR1 and CXCR2. By blocking these receptors, Ladarixin inhibits neutrophil recruitment and inflammatory responses. It is under investigation for the treatment of inflammatory airway diseases such as chronic obstructive pulmonary disease (COPD) and asthma. -
CXCR antagonist
LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory properties. It binds to CXCL12 with a Ki of 267 nM, thereby preventing its interaction with the CXCR4 receptor. LIT-927 is a valuable tool for studying CXCL12/CXCR4-mediated signaling in inflammatory and immune-related conditions. -
CXCR4 Antagonist
Nef-M1 is a CXCR4 antagonist peptide derived from the myristoylated protein encoded by the nef gene in HIV. It induces apoptosis by enhancing caspase-3 levels in cancer cells and inhibits critical processes associated with tumor progression, including angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 reduces levels of VEGF-A, phosphorylated GSK-3β, and vimentin while promoting E-cadherin expression. This compound is valuable for research applications focused on colorectal cancer and breast cancer. -
Anti-CXCR4 Antibody
LY-2624587 is a humanized IgG4 monoclonal antibody that antagonizes CXCR4. By blocking the interaction between SDF-1 and CXCR4, it inhibits SDF-1-induced GTP binding, significantly reducing cell migration and promoting apoptosis in human lymphoma and leukemia cells. Additionally, LY-2624587 impedes CXCR4 and SDF-1-mediated signaling pathways, including the activation of MAPK and AKT. This reagent is valuable for research applications involving human hematological malignancies, particularly acute myeloid leukemia (AML). -
CXCR4 Antagonist.
BPRCX807 is a selective and potent antagonist of the CXC chemokine receptor type 4 (CXCR4). It effectively inhibits CXCL12-mediated phosphorylation of ERK and Akt, leading to significant suppression of primary tumor growth. This compound is applicable for research in hepatocellular carcinoma, providing insights into its therapeutic potential in cancer treatment. -
CXCR4 Inhibitor
Hit 14 is a selective inhibitor of C-X-C chemokine receptor type 4 (CXCR4), demonstrating an IC50 value of 254 nM. This compound effectively inhibits the migration and invasion of MDA-MB-231 cells, highlighting its potential in cancer research. Furthermore, Hit 14 modulates Akt phosphorylation and exhibits anti-inflammatory properties, demonstrating efficacy in reducing ear swelling and damage in mouse models. Its diverse biological activities make it a valuable tool for studies related to cancer metastasis and inflammation. -
CXCR Inhibitor
Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications. -
CXCR Inhibitor
Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies. -
Stable Isotope
Kynurenic acid-d5 is a deuterium-labeled analog of kynurenic acid, an endogenous metabolite of tryptophan. It acts as a broad-spectrum antagonist of NMDA and glutamate receptors, as well as the α7 nicotinic acetylcholine receptor. Additionally, kynurenic acid-d5 serves as an agonist for GPR35/CXCR8, making it valuable in studies related to neuropharmacology and neurotransmitter signaling pathways. This stable isotope is ideal for tracing and characterization studies in metabolic research. -
CXCR-4 Inhibitor
SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions. -
CXCR2 Agonist
Ac-Pro-Gly-Pro-OH acts as a CXCR2 agonist and is an endogenous degradation product of extracellular collagen. This compound demonstrates significant bactericidal activity through hydrogen peroxide generation and plays a role in inhibiting pulmonary inflammation while reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH promotes the secretion of IFN-γ and suppresses the levels of pro-inflammatory cytokines such as TNF-α and IL-6 in leukocytes. It is relevant for research applications in sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcers, notably influencing neutrophil behavior and tissue remodeling processes. -
CXCR2 Antagonist
Elubrixin tosylate is a selective and reversible antagonist of the CXCR2 receptor, functioning as an IL-8 receptor antagonist. This compound effectively inhibits neutrophil CD11b upregulation with an IC50 of 260.7 nM and neutrophil shape change with an IC50 of 310.5 nM. Its biological activity positions Elubrixin tosylate as a valuable tool in research aimed at understanding and treating inflammatory diseases, including inflammatory bowel disease and airway inflammation. -
CXCR2 Antagonist
Elubrixin is a potent and selective CXCR2 antagonist, functioning as a competitive and reversible inhibitor of the IL-8 receptor. It effectively impedes neutrophil CD11b upregulation with an IC50 of 260.7 nM and inhibits shape change with an IC50 of 310.5 nM. This compound is valuable in the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation, facilitating insights into pathophysiological mechanisms and therapeutic interventions. -
CXCR2 Antagonist
Elubrixin hydrochloride is a potent, selective CXCR2 antagonist that operates as a competitive, reversible inhibitor of the IL-8 receptor. It effectively inhibits neutrophil CD11b upregulation and shape change, with an IC50 of 260.7 nM and 310.5 nM, respectively. This compound is valuable for research applications related to inflammatory diseases, including inflammatory bowel disease and airway inflammation. -
CXCR4 Antagonist
Burixafor hydrobromide is a potent CXCR4 antagonist with a pIC50 of 7.4, effectively inhibiting the binding of CXCL12 to the CXCR4 receptor. This compound antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, thereby obstructing the downstream Gαᵢ-mediated inhibition of cAMP signaling. Burixafor hydrobromide is utilized in research for mobilizing CD34+ hematopoietic stem/progenitor cells from the bone marrow to peripheral blood, making it valuable in studies related to autologous hematopoietic stem cell transplantation. -
Antagonist
Peptide E5 is an antagonist that targets the CXCR4/CXCL12 signaling axis. By blocking this interaction, Peptide E5 downregulates CXCR4 expression and inhibits the phosphorylation of key downstream proteins, Akt and Erk, leading to apoptosis in breast cancer cells. Additionally, Peptide E5 suppresses cellular migration and adhesion, as well as the recruitment of endothelial progenitor cells, thereby inhibiting tumor angiogenesis. This peptide is a valuable tool for research related to breast cancer and tumor microenvironment interactions. -
CXCR4 Antagonist
Peptide R analogue 10 is a potent CXCR4 antagonist, demonstrating enhanced antagonistic activity, specificity, and plasma stability compared to its predecessor, Peptide R. This compound effectively inhibits CXCL12-mediated cell migration, ERK phosphorylation, and CXCR4 internalization. Peptide R analogue 10 is valuable for research applications involving CXCR4 overexpression in models of leukemia and colon cancer. -
Bone Marrow Mesenchymal Stem Cell Inducer
Herpetin is an active lignan that functions as a bone marrow mesenchymal stem cell inducer. It activates the SDF-1/CXCR4 axis and the Wnt/β-catenin signaling pathway, promoting stem cell recruitment and differentiation. This compound is relevant for research applications focused on acute liver injury and related regenerative processes. -
CXCR4/STAT3 Inhibitor
Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development. -
RDC-related Molecule
NOTA-NHS ester is a chelating agent that allows for the creation of radiolabeled compounds, specifically through coupling with T140 to form NOTA-T140. This compound can then be radiolabeled with Al[18F], enabling visualization of tumor uptake that correlates with CXCR4 expression levels. Al[18F]NOTA-T140 is particularly valuable for PET imaging studies of tumors. Additionally, NOTA-NHS ester serves as a versatile tool for fluorescent labeling in various biological applications. -
CXCR4 Targeting Peptide
Pentixafor is a synthetic peptide that targets the CXCR4 receptor, playing a critical role in various cellular processes, including cell migration and signaling. This compound can be labeled with 68Gallium (68Ga), enabling its application in positron emission tomography (PET) imaging for assessing CXCR4 expression in vivo. Additionally, Pentixafor serves as a vital component in the development of Radionuclide-Drug Conjugates (RDCs) for targeted cancer therapies. -
Endoradiotherapeutic vector
Anditixafortide is a CXCR4-targeting peptide derivative that functions as an endoradiotherapeutic vector. This reagent is primarily utilized in the synthesis and research of Radionuclide-Drug Conjugates (RDCs), leveraging its ability to selectively target CXCR4-expressing cells. Its application is significant in the field of targeted cancer therapies, facilitating precise delivery of therapeutic radionuclides to tumor sites. -
Liposome
DOTA Conjugated JM#21 derivative 7 is a CXCR4-targeting peptide conjugated with DOTA, designed for the synthesis of radioligands. When radiolabeled as 177Lu-DOTA, it demonstrates superior targeting of CXCR4-expressing tumors while exhibiting minimal uptake in non-targeted organs, except for the kidneys. This compound is ideal for research applications involving Radionuclide-Drug Conjugates (RDCs), facilitating advancements in targeted radiotherapy. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
CXCR4 Antagonist
Mavorixafor trihydrochloride is a potent and selective antagonist of the CXCR4 receptor, exhibiting an IC50 of 13 nM in inhibiting CXCR4 125I-SDF binding. This compound has demonstrated significant antiviral activity by inhibiting the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs, with IC50 values of 1 nM and 9 nM, respectively. Mavorixafor trihydrochloride is applicable in research studying WHIM syndrome and various CXCR4-related biological processes. -
CCR7 and CXCR2 Antagonist
Cosalane is a dual antagonist of the chemokine receptors CCR7 (IC50 = 2.43 μM) and CXCR2 (IC50 = 0.66 μM). This compound effectively inhibits HIV replication across a variety of strains, including HIV-1, HIV-2, Rauscher murine leukemia virus, as well as herpes simplex viruses HSV-1 and HSV-2, and human cytomegalovirus. Cosalane disrupts the interaction between gp120 and CD4, inhibiting signaling downstream of CCR7 in response to its ligands CCL19 and CCL21. Research applications include studies on HIV and the potential modulation of acute graft-versus-host disease in allogeneic hematopoietic stem cell transplantation. -
CXCR4 Antagonist
TC14012 is a peptidomimetic antagonist targeting the chemokine receptor CXCR4, exhibiting a high level of selectivity with an IC50 of 19.3 nM. In addition, TC14012 acts as a potent agonist for CXCR7, demonstrating an EC50 of 350 nM in β-arrestin 2 recruitment assays. This compound is utilized in research focused on HIV and cancer therapy, showcasing its potential in modulating chemokine signaling pathways. -
CXCR4 Antagonist
FC131 TFA is a potent CXCR4 antagonist that effectively inhibits the binding of [125I]-SDF-1 to CXCR4, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-HIV activity, making it a valuable tool for research in HIV treatment and other CXCR4-related studies. Its ability to disrupt CXCR4 signaling can be explored in various biological contexts, including cancer metastasis and immune response regulation. -
CXCR4 Antagonist
AMD 3465 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of both the 12G5 monoclonal antibody and CXCL12AF647 to CXCR4, demonstrating IC50 values of 0.75 nM and 18 nM in SupT1 cells, respectively. Additionally, AMD 3465 significantly impedes the replication of X4-tropic HIV strains, with IC50 values ranging from 1 to 10 nM, while showing no activity against CCR5-using (R5) viruses. This compound is suitable for research applications focusing on HIV treatment and CXCR4-related signaling pathways. -
CXCR4 Antagonist
KRH-3955 hydrochloride is a potent CXCR4 antagonist that effectively inhibits the binding of SDF-1α to CXCR4 with an IC50 of 0.61 nM. This compound demonstrates strong selectivity and efficacy against X4 HIV-1, with an EC50 ranging from 0.3 to 1.0 nM. KRH-3955 hydrochloride is suitable for research applications focused on HIV-1 pathogenesis and CXCR4-related signaling pathways. -
CXCR4 Antagonist
FC131 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. Due to its mechanism of action, FC131 demonstrates significant anti-HIV activity, making it a valuable tool for research into HIV pathogenesis and potential therapeutic interventions. -
Stable Isotope
Plerixafor-d4 is a deuterated derivative of Plerixafor, a selective antagonist of the CXCR4 receptor with an IC50 of 44 nM. This compound serves as an immunostimulant and is known for its ability to mobilize hematopoietic stem cells (HSCs). Additionally, Plerixafor has demonstrated efficacy in inhibiting HIV-1 and HIV-2 replication, with an EC50 ranging from 1 to 10 nM. Plerixafor-d4 is useful in research applications requiring stable isotopes for tracking and quantification purposes. -
HIV-1 Entry Inhibitor
RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies. -
CXCR4 Antagonist
CXCR4 antagonist 7 is a potent CXCR4 antagonist with an IC50 of 9.3 nM. It effectively inhibits CXCR4 receptor activity, making it a valuable tool in the investigation of HIV infection, inflammatory diseases, cancer, and WHIM syndrome. This compound provides essential insights into the roles of CXCR4 signaling in various pathological conditions. -
CXCR Inhibitor
AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development. -
CXCR4 Antagonist
CXCR4 Antagonist 4 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 of 24 nM. It demonstrates enhanced permeability as assessed by PAMPA and has reduced activity on CYP 2D6. This compound is particularly effective in inhibiting the entry of human immunodeficiency virus, with an IC50 value of 7 nM, making it a valuable tool for research in virology and therapeutic development targeting CXCR4-mediated pathways. -
CXCR Antagonist
GSK812397 is a potent CXCR4 antagonist that functions by inhibiting the CXC chemokine receptor 4, a critical co-receptor for HIV-1 entry into host cells. This compound has demonstrated significant biological activity, making it a promising candidate for HIV treatment research. Its ability to suppress the replication of various late cytopathic viruses marks GSK812397 as a valuable reagent in the development of innovative anti-HIV therapies. Additionally, scalable synthetic routes enable efficient production, ensuring sufficient quantities for comprehensive investigation. -
CXCR Antagonist
CXCR4 antagonist 1 is a selective antagonist of the chemokine receptor CXCR4. It exhibits significant anti-HIV activity by inhibiting the interaction of CXCR4 with its ligands, thereby blocking viral entry into host cells. This compound is valuable in research focused on HIV pathogenesis and the development of therapeutic strategies targeting CXCR4. -
CXCR4 Antagonist
HF50731 is a potent antagonist of CXCR4, demonstrating a binding affinity with an IC50 value of 19.8 nM. This compound effectively inhibits key biological processes such as calcium mobilization and cell migration, with IC50 values of 119.2 nM and 621.4 nM, respectively. Additionally, HF50731 demonstrates the ability to inhibit HIV-1 infection through CXCR4 coreceptor blockade, achieving an IC50 of 1.5 μM. HF50731 is valuable for research in immunology, virology, and cancer biology focused on CXCR4 signaling pathways. -
CXCR Inhibitor
AMD-3329 is a selective CXCR4 inhibitor that targets the chemokine receptor involved in HIV-1 and HIV-2 entry into host cells. By obstructing CXCR4, AMD-3329 effectively inhibits viral replication, making it a valuable tool in HIV research. This compound is suitable for studies focused on developing therapeutic strategies against X4-tropic HIV strains and understanding the mechanisms of viral entry and infection. -
HIV Inhibitor
KRH-3955 is a potent CXCR4 antagonist that demonstrates significant anti-HIV-1 activity, particularly against X4 strains. It effectively inhibits the replication of various X4 HIV-1 clinical isolates and is active against recombinant strains with resistance mutations in reverse transcriptase, protease, and tyrosinase. KRH-3955 disrupts the binding of SDF-1alpha to CXCR4, thereby interfering with calcium signaling through this receptor, along with inhibiting antibody binding to CXCR4. With an oral bioavailability of 25.6% in rats, KRH-3955 has shown efficacy in vivo, making it a valuable tool for HIV research. -
CXCR2/CCR7 Antagonist
CXCR2/CCR7 antagonist-1 is a potent dual antagonist of the chemokine receptors CXCR2 and CCR7, exhibiting IC50 values of 0.0046 μM and 0.0014 μM, respectively. This compound serves as a valuable tool in the investigation of cancer metastasis and the mechanisms underlying autoimmune diseases, facilitating the study of therapeutic strategies targeting these pathways. Its efficacy in inhibiting both receptors makes it suitable for a range of biochemical and pharmacological research applications. -
CCR6/CXCR2 Antagonist
SQA1 is a squaramide derivative that functions as a CCR6 and CXCR2 antagonist, displaying a dissociation constant (Kd) of 250 nM. It effectively occupies the intracellular pocket, overlapping with the G protein binding site, which helps stabilize the closed conformation of the receptor. This compound is useful in research applications targeting chemokine receptor signaling pathways and their roles in inflammatory responses and immune cell trafficking. -
CCR5/CXCR3 Inhibitor
CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial. -
CXCR Antagonist
ACT-1004-1239 is a selective antagonist of the CXCR7 receptor, exhibiting a potent inhibitory effect with an IC50 value of 3.2 nM. This compound is primarily utilized in research focused on chemokine signaling pathways and is relevant in studies investigating disorders related to the immune system and cancer. Its oral bioactivity makes it an attractive candidate for in vivo investigations targeting CXCR7-mediated pathways. -
CXCR4 Receptor Agonist
NUCC-390 dihydrochloride is a selective small-molecule agonist of the CXCR4 receptor. It promotes the internalization of CXCR4 receptors and exhibits effects that are opposite to those of conventional CXCR4 antagonists. This compound has demonstrated the potential to enhance nerve recovery following neurodegeneration in vivo, making it a valuable tool for research in neurobiology and therapeutic applications targeting nerve regeneration. -
CXCR3 Antagonist
ACT-777991 is a selective antagonist of the CXCR3 receptor, demonstrating oral bioavailability. This compound effectively inhibits the migration of activated T cells in response to CXCL11, making it a useful tool for studying immune responses and inflammatory conditions. Its stability in microsomes and hepatocytes across various animal models further supports its potential applications in pharmacological research related to autoimmune diseases and cancer immunotherapy. -
ACKR7 Agonist
VUF11207 fumarate is a selective agonist of the ACKR7 receptor (formerly known as CXCR7). This compound effectively inhibits CXCL12-induced osteoclastogenesis and bone resorption by preventing ERK phosphorylation. VUF11207 fumarate is valuable for research targeting bone metabolism and related pathologies, making it a key tool for studying the role of ACKR7 in bone homeostasis and signaling pathways. -
CXCR3 Agonist
PS372424 hydrochloride is a selective agonist of the CXCR3 receptor, a key player in immune response modulation. This compound exhibits anti-inflammatory properties by inhibiting human T-cell migration, making it valuable for research into inflammatory diseases, particularly in models of arthritic inflammation. Its ability to target CXCR3 offers insight into the therapeutic potential for treating conditions characterized by dysregulated T-cell activity.
