Overview | Theracemicmixtureofacell-permeablepyridocarbazolo-cyclopentADIenylRutheniumcomplexthatactsasareversIBLe,ATP-competitive,andhighlypotentinhibitorofGSK-3(IC50=0.4and0.6nMforGSK-3αandGSK-3β,respectively)with~5-foldselectivityoverPIM-1kinase(IC50=3nM).Studiesusingisolatedenantiomershaveshownthatthe(R)-enantiomerisGSK-3-selective(IC50=0.35,0.55,and35nMforGSK-3αGSK-3β,andPim-1,respectively)andinterfereswithnormalzebrafishembryodevelopment(1μM),whilethe(S)-enantiomerisPim-1-selective(IC50=80,90,and3nMforGSK-3αGSK-3β,andPim-1,respectively)andexhibitsnoeffectinembryodevelopmentatthesamedosage. |