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GNF4877

CAS No. : 2041073-22-5

MCE 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.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  CHIR-99021  |  SB 216763  |  Harmine  |  AR-A014418  |  TDZD-8  |  Kenpaullone  |  GSK 3 Inhibitor IX  |  AZ191  |  Cromolyn sodium  |  R547  |  GSK-626616  |  Protein kinase inhibitors 1 hydrochloride  |  tBID  |  SB 415286  |  IM-12  |  Indirubin-3'-monoxime  |  1-Azakenpaullone  |  AZD2858  |  BIO-acetoxime  |  CP21R7  |  Bikinin  |  ID-8  |  LDN-192960 hydrochloride  |  Mirk-IN-1  |  GSK-3β inhibitor 1  |  hSMG-1 inhibitor 11j  |  AZ-Dyrk1B-33

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