GNF4877,2041073-22-5

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GNF4877

CAS No. : 2041073-22-5

MCE 国际站：GNF4877

产品活性：GNF4877是 DYRK1A 和 GSK3β 的有效抑制剂，IC₅₀ 值分别为 6 nM 和 16 nM，可导致 NFATc 核输出受阻并增加 β 细胞增殖 (对小鼠 β (R7T1) 细胞的 EC₅₀ 值为 0.66 μM)。

研究领域：Protein Tyrosine Kinase/RTK  |  Stem Cell/Wnt  |  PI3K/Akt/mTOR

作用靶点：DYRK  |  GSK-3

In Vitro: High glucose concentrations and glucokinase activators (GKAs) increase Ca²⁺ signalling in β-cells, and increase intracellular Ca²⁺ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC₅₀ for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca²⁺ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca²⁺ channel activator) show additive activity with GNF4877.

In Vivo: GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.

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