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ZSTK474

CAS No. : 475110-96-4

MCE 站：ZSTK474

产品活性：ZSTK474 是一种 ATP 竞争性的泛 I 类 PI3K 抑制剂，抑制 P13Kα，PI3Kβ，PI3Kδ 和 PI3Kγ，IC₅₀ 分别为 16 nM，44 nM，4.6 nM 和 49 nM。

研究领域：PI3K/Akt/mTOR  |  Autophagy

作用靶点：PI3K  |  Autophagy

In Vitro: Lineweaver-Burk plot analysis revealed that ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. The K_i values determined for the four PI3K isoforms showed that ZSTK474 inhibited the PI3Kδ isoform most effectively with a K_i of 1.8 nM, whereas the other isoforms are inhibited with 4-10-fold higher K_i values. Therefore, ZSTK474 should be regarded as a pan-PI3K inhibitor. We also determined the IC₅₀ values for inhibiting the four PI3K isoforms with ZSTK474 ａnd LY294002. The IC₅₀ values of ZSTK474 (16, 44, 4.6 ａnd 49 nM for PI3Kα, PI3Kβ, PI3Kδ ａnd PI3Kγ, respectively) are shown to be consistent with the K_i values (6.7, 10.4, 1.8 ａnd 11.7 nM for PI3Kα, PI3Kβ, PI3Kδ ａnd PI3Kγ, respectively), which further supported the idea that ZSTK474 inhibits PI3Kδ most potently. Even at a concentration of 100 µM, ZSTK474 inhibits mTOR activity rather weakly.

In Vivo: In mice subjected to MCAO, treatment with ZSTK474 is tested at dosages of 50, 100, 200, ａnd 300 mg/kg. Since the 200 mg/kg dose produces significant improvement ａnd no obvious toxic effects (P<0.01), mice are treated with ZSTK474 at a dose of 200 mg/kg/day daily for three post-MCAO days during the remaining experiments of this study. Neurological function is examined in mice suffered from MCAO followed by 24, 48, ａnd 72 h of reperfusion. In the ZSTK474 group, neurological function scores are significantly better than the control group except the corner test.

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