sb225002

Description: SB225002 (SB 225002; SB-225002) is a novel, potent, and selective non-peptide antagonist of chemokine receptor CXCR2 with potential anti-inflammatory activity. It inhibits CXCR2 with an IC50 of 22 nM for inhibiting the binding of interleukin 125I-IL-8 to CXCR2. SB 225002 showed > 150-fold selectivity over CXCR1 and four other 7-TMRs tested. In vitro, SB 225002 potently inhibited human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha. In vivo, SB 225002 selectively blocked IL-8-induced neutrophil margination in rabbits. The present findings suggest that CXCR2 is responsible for neutrophil chemotaxis and margination induced by IL-8. SB225002 is also reported to be a mitotic inhibitor that promotes mitotic catastrophe in chemo-sensitive and -resistant ovarian cancer cells independent of p53 status in vitro. SB225002 induces apoptosis in both wild-type and p53-deficient ovarian cancer (OVCA) cells through alternative mechanisms. This selective antagonist will be a useful tool compound to define the role of CXCR2 in inflammatory diseases where neutrophils play a major role.

References: J Biol Chem. 1998 Apr 24; 273(17):10095-8; Cancer Res. 2006 Mar 15; 66(6):3071-7; Surgery. 2014 Apr; 155(4):640-9.

SB225002; SB 225002; SB225002;

Chemical Name: 1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea

SMILES Code: O=C(NC1=CC=C([N+]([O-])=O)C=C1O)NC2=CC=CC=C2Br

Exact Mass: 350.98547