tcsc0139 SB 216763

SB 216763 is potent and selective and ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor, with an IC₅₀ value of 34.3 nM for GSK-3α and GSK-3β, respectively.

IC50 & Target: IC50: 34.3 nM (GSK-3α), 34.3 nM (GSK-3β)^[5]

In Vitro: SB-216763 (10-20 µM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 µM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 µM) can maintain J1 mESCs in a pluripotent state for more than a month^[2]. SB-216763 inhibits GSK-3 with IC₅₀ of 34 nM^[3]. SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β^[5].

In Vivo: SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis^[1]. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E₁₀₀ or Geni₁₀₀ reverses the ceiling effect because these agents significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO^[4].