cxcr2-in-2

(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).

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

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.

Ladarixin (DF 2156A free base) is an orally active, non-competitive CXCR1/CXCR2 allosteric inhibitor that suppresses AKT, NF-κB, and angiogenesis, thereby slowing the progression of experimental human melanoma. It may be employed in research concerning COPD, asthma, and melanoma.

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].

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.

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].

Anti-CXCL8/IL-8 Antibody is a humanized monoclonal antibody targeting the chemokine CXCL8 (Interleukin-8, IL-8). CXCL8 is a pro-inflammatory chemokine frequently overexpressed in the tumor microenvironment, which promotes tumor angiogenesis, survival, proliferation, and migration by binding to its G protein-coupled receptors, CXCR1 and CXCR2. This antibody effectively neutralizes extracellular CXCL8, blocking its interaction with CXCR1/2 and subsequently disrupting the paracrine and autocrine signaling loops driven by CXCL8. This mechanism inhibits tumor-associated vascularization and diminishes tumor cell resistance to conventional therapies, making it a critical tool for researching solid tumor progression, metastasis, and microenvironmental modulation.