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)。

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC 50 s of 6?nM and 16?nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC 50 of 0.66?μM for mouse β (R7T1) cells).

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GSK3β 16 nM (IC50) DYRK1A 6 nM (IC50

High glucose concentrations and glucokinase activators (GKAs) increase Ca signalling in β-cells, and increase intracellular Ca 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 Ca with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca channel activator) show additive activity with GNF4877. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372.

In Vitro: DMSO : 4.17 mg/mL (8.43 mM; Need ultrasonic and warming)配制储备液