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Laduviglusib

CAS No. : 252917-06-9

MCE 国际站：Laduviglusib

产品活性：Laduviglusib (CHIR-99021) 是一种有效的，选择性的，具有口服活性的 GSK-3α/β 抑制剂，IC₅₀ 为 10 nM 和 6.7 nM。Laduviglusib 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib 能诱导细胞自噬 (autophagy)。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Autophagy

作用靶点：GSK-3  |  Wnt  |  β-catenin  |  Autophagy

In Vitro: Laduviglusib (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC₅₀ of 4.9 μM.
Laduviglusib (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells.
Laduviglusib (3 μM, 4 days) inhibits ES cell differentiation into neural cells.
Laduviglusib (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes.
Laduviglusib (2.5 μM, 24 h) protects Lgr5+ cells against radiation-induced apoptosis.

In Vivo: Laduviglusib (30 mg/kg, p.o ) rapidly lowers plasma glucose.
Laduviglusib (2 mg/kg, i.p.) protects mice against radiation-induced lethal GI injury.

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