Catalog No.
Product Name
Application
Product Information
Citations
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CXCR
CX4338 is a selective inhibitor of the chemokine receptor CXCR2, targeting CXCL8-mediated pathways. This compound effectively inhibits CXCR2-mediated cell migration by suppressing β-arrestin-2 recruitment and receptor internalization while enhancing MAPK activation. CX4338 demonstrates potent inhibition of CXCL8-induced chemotaxis in CXCR2-overexpressing cells and human neutrophils. In vivo studies have shown that CX4338 significantly reduces LPS-induced neutrophil infiltration in mouse bronchoalveolar lavage fluid, highlighting its potential for research in inflammatory and immune responses. -
CXCR4 Inhibitor
TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression. -
CXCR4 Antagonist
CXCR4 antagonist 6 is a potent inhibitor of the CXCR4 receptor, displaying an IC50 value of 79 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, thereby significantly reducing CXCL12/CXCR4-mediated cell migration. Additionally, CXCR4 antagonist 6 demonstrates substantial efficacy in in vivo cancer metastasis models, making it a valuable tool for research in cancer biology and therapeutic development. -
CXCR Antagonist
CXCR4 Antagonist 2 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 value of 47 nM. This compound effectively inhibits CXCR4-mediated signaling, making it a valuable tool for studying its role in various biological processes, including cancer metastasis, immune cell trafficking, and HIV infection. Its selective properties make it suitable for research applications aimed at understanding CXCR4 functions and developing therapeutic strategies targeting this receptor. -
CXCR4 Antagonist
KRH-1636 is a potent CXCR4 antagonist, primarily targeting the CXCR4 receptor. This compound plays a significant role in HIV-1 research by inhibiting the interaction between the virus and the CXCR4 receptor, which is crucial for viral entry into host cells. KRH-1636 serves as a valuable tool for studying the mechanisms of HIV-1 infection and for exploring therapeutic strategies aimed at disrupting CXCR4-mediated pathways. -
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. -
CXCR3 antagonist
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments. -
CXCR3 antagonist
AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3. -
non-peptide CCR1 antagonist
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. -
CXCR4 antagonist
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. -
CXCR4 antagonist
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM. -
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. - Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
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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. - 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.
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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. -
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
CXCR2 antagonists
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. -
CXCR2 antagonist
SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury. -
EGFR inhibitor
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
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GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. -
CXCR2 receptor antagonist
Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
