AS-041164

A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive, and isoform-selctive PI3-K inhibitor (γ isoform IC50 = 0.07 µ M, (α isoform IC50 = 0.24 µ M, (β isoform IC50 = 1.45 µ M, and (&delta, isoform IC50 = 1.70 µ M) with little or no activity against a panel of 38 other commonly studied kinases (<20% inhibition at 1.0 µ M). Exhibits similar pharmacokinetics as LY 294002 via oral administration, but is 3-times as potent (ED50 = 27.35 mg/kg, p.o.) in blocking rhRNATES-induced neutrophil peritoneal recruitment in mice in vivo. Also reported to exhibit significant in vivo prophylactic efficacy against carrageenan-induced tissue swelling in a rat paw edema model (100 mg/kg, p.o)

6318-41-8

C₁₄H₈FNO₄S

Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS.