Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
CXCR2 receptor antagonist
Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.
