cxcr2-in-1

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

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.

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

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.

(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-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).

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).

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].

Corydalmine hydrochloride is a chemical compound that suppresses spore germination in certain plant pathogenic and saprophytic fungi [1], serves as an effective oral analgesic agent with potent activity [2], and mitigates Vincristine-induced neuropathic pain in mice through the inhibition of an NF-κB-dependent CXCL1/CXCR2 signaling pathway [3].

(Rac)-Reparixin serves as an isomer of Reparixin and is used as a control compound in experiments. Reparixin acts as a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2, with IC50 values of 1 nM and 100 nM respectively.