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. 2012 May 21;2012:930710. doi: 10.1155/2012/930710

Table 3.

List of known positive regulators of GSK-3β.

Activator Activation potency Mode of activation Notes
Celecoxib IC50 = 3.5 μM Inhibits PDK phosphorylation of Akt COX-2 inhibitor [100].
Staurosporine IC50 = 0.22 μM Inhibits PDK phosphorylation of Akt General kinase inhibitor (including PKA/PKC) [101, 103, 104].
Trichostatin A Unknown Induces Akt dephosphorylation HDAC inhibitor acts through PP1 [105].
Curcumin Unknown Akt dephosphorylation Direct target not known [102].
Akt/protein kinase B
signaling inhibitor-2 (API-2)
Unknown Suppresses Akt kinase activity and activation Does not affect upstream Akt activators [106].
Wortmannin IC50 = 5 nM Inhibits PI3-Kinase Indirect effect on GSK-3β [97, 98].
LY294002 IC50 = 1.4 μM Inhibits PI3-Kinase Likely affects ATP binding to kinase [98, 99].
Rapamycin Unknown Potentially inhibits S6K1 mTOR pathway can also inhibit GSK3 [107, 108].
Differentiation-inducing
factors (DIFs)
Unknown Enhances GSK-3β kinase activity and promotes nuclear localization Reduces inhibitory phosphorylation and enhances activating phosphorylation [111, 112].
Retinoids Unknown Reduces inhibitory phosphorylation of GSK-3β Promotes GSK-3β-dependent cyclin D1 degradation [80, 109].