GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively
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产品名称 | GSK-3 ↓ ↑ | GSK-3α ↓ ↑ | GSK-3β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD2858 |
+
GSK-3, IC50: 68 nM |
99%+ | |||||||||||||||||
Bikinin | ✔ | 99%+ | |||||||||||||||||
GSK 3 Inhibitor IX |
++++
GSK-3, IC50: 5 nM |
99%+ | |||||||||||||||||
AZD1080 |
+++
GSK-3α, IC50: 6.9 nM |
++
GSK-3β, IC50: 31 nM |
99%+ | ||||||||||||||||
BIO-acetoxime |
+++
GSK-3α, IC50: 10 nM |
+++
GSK-3β, IC50: 10 nM |
95% | ||||||||||||||||
SB-216763 |
++
GSK-3α, IC50: 34.3 nM |
++
GSK-3β, IC50: ~34.3 nM |
98% | ||||||||||||||||
SB 415286 |
+
GSK-3α, IC50: 78 nM |
+
GSK-3β, IC50: ~78 nM |
99%+ | ||||||||||||||||
CHIR-98014 |
++++
GSK-3α, IC50: 0.65 nM |
++++
GSK-3β, IC50: 0.58 nM |
99%+ | ||||||||||||||||
LY2090314 |
++++
GSK-3α, IC50: 1.5 nM |
++++
GSK-3β, IC50: 0.9 nM |
99%+ | ||||||||||||||||
CHIR 99021 |
+++
GSK-3α, IC50: 10 nM |
++++
GSK-3β, IC50: 6.7 nM |
99%+ | ||||||||||||||||
TDZD-8 |
+
GSK-3β, IC50: 2 μM |
99%+ | |||||||||||||||||
Indirubin |
+
GSK-3β, IC50: 0.6 μM |
99%+ | |||||||||||||||||
IM-12 |
++
GSK-3β, IC50: 53 nM |
99%+ | |||||||||||||||||
TWS119 |
++
GSK-3β, IC50: 30 nM |
99%+ | |||||||||||||||||
1-Azakenpaullone |
+++
GSK-3β, IC50: 18 nM |
99%+ | |||||||||||||||||
AR-A014418 |
++
GSK-3β, Ki: 38 nM |
99%+ | |||||||||||||||||
Tideglusib |
+
GSK-3β, IC50: 60 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | GNF4877 is a highly potent inhibitor of DYRK1A and GSK3β, with IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the prevention of nuclear factor of activated T-cells (NFATc) nuclear export and enhanced β-cell proliferation (with an EC50 of 0.66 μM for mouse β (R7T1) cells) [1]. |
体内研究 | Elevated glucose levels and glucokinase activators (GKAs) enhance Ca2+ signaling in β-cells, leading to increased intracellular Ca2+ levels, which in turn activate calcineurin and facilitate the nuclear translocation of NFATc proteins. Remarkably, GNF4877 concentrations (0.1 μM, 0.3 μM), significantly lower than the EC50 for β-cell proliferation, induce proliferation in the presence of high glucose or pharmacological glucokinase activators. Additionally, augmenting intracellular Ca2+ levels with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) exhibits additive effects with GNF4877 [1]. |
体外研究 | Elevated glucose levels and glucokinase activators (GKAs) enhance Ca2+ signaling in β-cells, leading to increased intracellular Ca2+ levels, which in turn activate calcineurin and facilitate the nuclear translocation of NFATc proteins. Remarkably, GNF4877 concentrations (0.1 μM, 0.3 μM), significantly lower than the EC50 for β-cell proliferation, induce proliferation in the presence of high glucose or pharmacological glucokinase activators. Additionally, augmenting intracellular Ca2+ levels with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca2+ channel activator) exhibits additive effects with GNF4877 [1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.02mL 0.40mL 0.20mL |
10.11mL 2.02mL 1.01mL |
20.22mL 4.04mL 2.02mL |
CAS号 | 2041073-22-5 |
分子式 | C25H27FN6O4 |
分子量 | 494.518 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 3 mg/mL(6.07 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |