CXCR

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.

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.

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.

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.

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.

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 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.

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.

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.

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.

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.

(±)-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.

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.

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.

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 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.

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.

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 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.

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.

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.

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.

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.

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.

9(R)-HODE is a monohydroxy fatty acid and an endogenous metabolite of linoleic acid, generated through the enzymatic actions of cyclooxygenase (COX) and lipoxygenase (LO). This compound is known to promote chemotaxis and elevate the expression of chemokine receptors CCR9 and CXCR4 in immune cells. Additionally, 9(R)-HODE effectively inhibits interleukin-6 (IL-6) release in primary human monocytes and suppresses CD3α- and CD28-induced proliferation in isolated human peripheral blood lymphocytes at a concentration of 25 μg/mL, making it a valuable tool for studying immune responses and inflammatory processes.

Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models.

VUF11207 is a potent agonist of the CXCR7 receptor, demonstrating a high affinity with a pKi of 8.1. This compound effectively induces the recruitment of β-arrestin2, with an pEC50 value of 8.8, and promotes the subsequent internalization of CXCR7, with an pEC50 of 7.9. VUF11207 is valuable for research applications focused on CXCR signaling pathways and β-arrestin-mediated processes.

Catenarin, an anthraquinone compound, serves as an inhibitor of CCR5 and CXCR4-mediated chemotaxis. It effectively reduces the phosphorylation of mitogen-activated protein kinases (p38 and JNK) and their upstream kinases (MKK6 and MKK7), as well as calcium mobilization. Catenarin demonstrates anti-inflammatory properties and inhibits leukocyte migration, contributing to its potential in diabetes research. Additionally, it exhibits significant antibacterial activity against Gram-positive bacteria and has been shown to prevent type 1 diabetes in nonobese diabetic mice.

UCUF-965 is a positive allosteric modulator of the chemokine receptor CXCR4. This compound enhances CXCL12-induced β-arrestin recruitment and cAMP signaling, promoting lymphoblast migration and inducing calcium flux without binding to the orthosteric CXCL12 site. UCUF-965 also modulates microRNA levels in fibroblasts by reducing miR-15b and miR-29a, while increasing miR-146a. Its capabilities in enhancing angiogenesis and accelerating wound healing make UCUF-965 a valuable tool in research focused on diabetic wound healing impairment.

YU241279 is a selective inhibitor of CXCR5, targeting the CXCL13-mediated signaling pathways. It effectively inhibits Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells, leading to reduced proliferation of lymphoma cells. In preclinical studies, YU241279 demonstrated a significant reduction in tumor burden within the peripheral blood and bone marrow of mice with lymphoma. This compound is suitable for research into angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma.