Uses
TWS119 has been used as glycogen synthase kinase-3β (GSK-3β) GSK3β inhibitor.
Uses
Acts as an ARMS-selective inihibitor, through GSK3 (Glucose Synthase Kinase 3) inhibition.
Definition
ChEBI: 3-[[6-(3-aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenol is a member of pyrroles.
General Description
A cell-permeable and potent inhibitor of GSK-3β (IC
50 = 30 nM). Binds to GSK-3β with high-affinity (K
d = 126 nM), leading to an increase in the level of β-catenin, a downstream substrate of GSK-3β in the Wnt signaling pathway. Shown to selectively induce neuronal differentiation in both pluripotent murine embryonal carcinoma cells (P19; 30-40% at 1 μM) and embryonic stem cells (D3; 50-60% at 400 nM).
Biological Activity
Inhibitor of glycogen synthase kinase-3 β (IC 50 = 30 nM). Induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
Biochem/physiol Actions
TWS119 favors the γδT cells survival and proliferation by activating the mammalian target of rapamycin (mTOR) pathway. It also promotes the expression of T-cell factor 1 (TCF1) and modulates cytokine production.
References
[1] ding s, wu t y h, brinker a, et al. synthetic small molecules that control stem cell fate. proceedings of the national academy of sciences, 2003, 100(13): 7632-7637.
[2] wu t y h, ding s. applying chemical tools to the discovery of novel regenerative medicine. drug discovery today: technologies, 2006, 3(3): 255-260.
