SX-517

SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC 50 =38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC 50 =60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model In Vitro SX-517 (compound 7) (0.1 nM-0.1 mM; 60 min) potently inhibits [35S]GTPγS binding induced by 10 nM CXCL8 with an IC50 of 60 nM. SX-517 (10 μM; 60 min) has inhibitory effect on the cell surface expression of CXCR2 in HEK293 cells. SX-517 (10 μM; 0-30 min) blocks CXCR2-mediated phosphorylation of ERK1/2 in HEK293 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HEK293 cells Concentration: 10 μM; with or without 100 ng/mL CXCL-8 Incubation Time: 0, 5, 15, 30 min Result: Completely blocked CXCL-8-induced phosphorylation of ERK1/2 by 30 min. In Vivo SX-517 (compound 7) (0.2 mg/kg; iv; single dose) significantly inhibits inflammation in an in vivo murine model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old) Dosage: 0.02 mg/kg, 0.2 mg/kg Administration: Intravenous injection; single dose Result: Significant reduction in cell count in the pouches of treated animals compared to the positive control cohort. Form:Solid IC50& Target:CXCR2 CXCR1

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