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 |