cxcr2

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor.

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

SCH 563705 is an orally available and highly potent CXCR2 and CXCR1 antagonist for the study of acute respiratory syndrome, chronic obstructive pulmonary disease, and inflammation.

SRT3190 is an antagonist of CXCR2.

SB225002 is a potent and selective CXCR2 antagonist inhibiting interleukin IL-8 binding to CXCR2.

SRT3109 is a CXCR2 ligand used in the treatment of chemokine mediated diseases and conditions.

Reparixin (Repertaxin) is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).

Danirixin (GSK1325756) is a potent antagonist of CXCR2 that inhibits IL-8 binding to CXCR2 (IC50: 12.5 nM).

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

Ac-Pro-Gly-Pro-OH is an acetyl-modified tripeptide compound that acts as a CXCR2 agonist, exhibiting bactericidal and anti-inflammatory activities. It inhibits apoptosis of immune cells, suppresses the production of pro-inflammatory cytokines, and has been utilized in studies of sepsis and lung inflammation.

AZD-5069 is an chemokine receptor 2 antagonist (CXCR2; IC50 = 0.79 nM).

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.

CXCR2/CCR7 antagonist-1 (compound 6) is a potent dual antagonist of CXCR2 and CCR7, with IC50 values of 0.0046 μM and 0.0014 μM, respectively. It is valuable for research in tumor metastasis and autoimmune diseases.

CXCR2-IN-2 (compound 68) is a highly selective CXCR2 antagonist (IC50=5.2 nM) with the advantages of blood-brain barrier penetration and oral bioavailability. It inhibits Gro-α-induced CD11b expression in human whole blood (IC50=0.04 μM).

CXCR2 antagonist 8 is a selective CXCR2 antagonist, which can be used for the treatment and prevention of insulin resistance.

CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.013 μM) and effective calcium mobilization (IC50 = 0.1 μM) [1].

CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.044 μM) and calcium mobilization (IC50 = 0.66 μM) [1].

CXCR2 antagonist 3 (compound 11h) is a highly effective inhibitor of CXC chemokine receptor 2 (CXCR2), displaying double-digit nanomolar potencies in inhibiting neutrophil infiltration into the air pouch. Additionally, it reduces neutrophil and MDSC infiltration while enhancing CD3+ T lymphocyte infiltration into Pan02 tumor tissues [1].

CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.044 μM) and effective calcium mobilization (IC50 = 0.66 μM) [1].

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy, exhibiting an IC50 value of 95 nM.