cxcr2

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 (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).

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.

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

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

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

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 4 (compound 7) is a highly potent inhibitor of CXCR2 with an IC50 of 0.13 μM and effectively inhibits the CXCL8-induced cytosolic calcium increase with an IC50 of 27 μM, demonstrating promising potential for anticancer research [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].

(R,R)-CXCR2-IN-2, a diastereoisomer of CXCR2-IN-2 (compound 68), is a brain-penetrant CXCR2 antagonist with a pIC50 of 9 in the Tango assay and 6.8 in the HWB Gro-α induced CD11b expression assay[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 8 is a potent and selective CXCR2 antagonist suitable for researching insulin resistance [1].

CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-fold selectivity over CXCR1 and greater than 1900-fold selectivity over all other chemokine receptors. Furthermore, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood, displaying an IC50 of 0.04 μM[1].

NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability.

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].

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.

AZ10397767 is a potent CXCR2 antagonist (IC50 = 1 nM). AZ10397767 significantly reduced the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

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

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.

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

SRT3190 is an antagonist of CXCR2.

Elubrixin is a interleukin 8 inhibitor and CXCR2 selective antagonist.

Elubrixin tosylate (SB-656933 tosylate) is a high-potency, selective, competitive, and reversible CXCR2 and IL-8 receptor antagonist. It effectively inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). This compound holds promise for studying inflammatory diseases, including inflammatory bowel disease and airway inflammation.