GSK-3𝜷: A Bifunctional Role in Cell Death Pathways

Table 4

Selected list of known GSK-3β inhibitors.

Inhibitor	Inhibition potency	Mode of inhibition	Notes
Beryllium	IC50 = 6 mM	Mg competitor	Also inhibits cdc2
Lithium	Ki =2 mM	Mg competitor
Anilino maleimides (SB216763, SB415286)	Ki = 10–30 nM	ATP competitor	Does not inhibit a range of other kinases
Arylpyrazolopyridazines; (e.g., 6-aryl pyrazole [3,4-b] pyridine 4)	IC50 = 0.8–150 nM	ATP competitor	Also inhibits CDK2
Bisindole maleimides (e.g., Ro 31-8220, GF 109203x)	IC50 = 5–170 nM	ATP competitor	Also inhibits PKC
Indirubins (6-bromoindirubin-3′-oxime, aka BIO)	IC50 = 5–50 nM	ATP competitor	Also inhibits CDKs
Paullones (alsterpaullone)	IC50 = 4–80 nM	ATP competitor	Also inhibits CDKs
Pseudosubstrate peptide	Ki = 0.7 mM	Substrate competitor	Specific