CXCR

AZD8797 is an allosteric non-competitive and orally active modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.

ML 145 is a selective GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM, but not for the related GPR55 orphan receptor. GPR35 is expressed by various cells of the immune system and it may has potential as a therapeutic target in inflammatory disease.

Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.

IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.

AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.

PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.

CXCR7 modulator 1 (compound 25) is a potent and orally bioavailable peptoid hybrid CXCR7 modulator, with a Ki of 9 nM.

AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.

Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.

UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.

AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.

Decursin is an anticancer agent, with potential anti-inflammatory activity.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.