资料参考

Description: IC50 Value:N/A LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K. in vitro: 100 μM LY303511 significantly reduced the fraction of cells in S phase. The proportion of cells in G2/M remained unchanged, indicating that cells were arrested in both G1 and G2/M. In contrast, rapamycin increased the G1 population by reducing the proportion of cells in both S and G2/M. The effects of 10 μM LY303511 and rapamycin on the reduction in S phase cells were additive to that of 10 μM LY303511 alone (P = 0.056) [1]. In MIN6 insulinoma cells, wortmannin (100 nM) had no effect on whole-cell outward K+ currents, but LY294002 and LY303511 reversibly blocked currents in a dose-dependent manner (IC50=9.0+/-0.7 microM and 64.6+/-9.1 microM, respectively). Western blotting confirmed the specific inhibitory effects of LY294002 and wortmannin on insulin-stimulated PI3K activity [2]. Both LY294002 and LY303511 increased the activity of protein kinase A (PKA). Moreover, PKA blockade by the small molecule inhibitor H89 decreased the LY294002/LY303511-mediated increase in GJIC [3]. in vivo: PND4 ovaries were cultured for 8 days in control medium or medium containing VCD (30 μM) in the presence or absence of LY303511 (20 μM). Incubation with LY303511 alone caused a reduction (P < 0.05) in primordial and small primary follicle numbers. On the other hand, whereas VCD alone depleted (P < 0.05) primordial and small primary follicle numbers, this depletion was not prevented by co-incubation with LY303511 [4]. Clinical trial: N/A