SB-225002
CXCR2 antagonist / Potent and selective CXCR2 receptor antagonist (IC50 = 22 nM). Displays >150-fold selectivity over CXCR1 receptors.1 Induces apoptosis in both wild-type and p53-deficient ovarian cancer cells (OVCA) via p53 activation and by inducing mitotic catastrophe.2 Blocks IL-8-mediated cellular effects such as oxidative stress-induced cellular senescence3 and neutrophil chemotaxis1. Inhibits HIV replication in lymphocytes and macrophages.4 Inhibits endothelial activation and leukocyte recruitment to cerebral microvessels during neuroinflammation.5
Biochemicals & reagents
182498-32-4
1) White et al. (1998), Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration; J.Biol.Chem. 273 10095 2) Du et al. (2013) SB225002 Promotes Mitotic Catastrophe in Chemo-Sensitive and -Resistant Ovarian Cancer Cells Independent of p53 Status In Vitro; PLoS One. 8 e54572 3) Shen et al. (2013), Interleukin-8 prevents oxidative stress-induced human endothelial cell senescence via telomerase activation; Int.Immunopharmacol. 16 261 4) Lane et al. (2001), Interleukin-8 Stimulates Human Immunodeficiency Virus Type 1 Replication and Is a Potential New target for Antiretroviral Therapy; J.Virol. 75 8195 5) Wu et al. (2015), CXCR2 is essential for cerebral endothelial activation and leukocyte recruitment during neuroinflammation; J.Neuroinflammation 12 98
-20°C
TARGET: GPCR -- PATHWAY: Cytokine; Apoptosis inducer; Senescence -- RESEARCH AREA: Neuroscience; Cellular stress; Cell death -- DISEASE AREA: Inflammation; AgeingNeurodegeneration