SB225002 182498-32-4

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Molecular Weight:

352.14 SB225002 is a potent, and Selective CXCR2 Antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

Biological Activity

In vitro, SB225002 inhibits GROα-stimulated calcium mobilization, and
potently inhibits human and rabbit neutrophil chemotaxis induced by both
IL-8 and GROalpha. SB 225002 substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. SB225002 also shows the antitumor activity as a microtubule inhibitor.


In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. In mouse intrahepatic cholangiocellular carcinoma model, SB225002 (1
mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. In addition, SB225002 also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models.

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Product Categories : GPCR & G Protein > CXCR Inhibitor