BRD0209 showed concentration-dependent inhibition of Tau with cellular EC50s of 1.76 μM, respectively, in SH-SY5Y cells using ELISA. Treatment of SH-SY5Y cells with BRD0209 (10 μM) significantly inhibited GSK3 kinase activity within 30 min, as seen in the decrease in phospho-CRMP2 and phospho-β-catenin. BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively).BRD0209 treatment caused a dramatic decrease in autophosphorylation at Tyr279 (pGSK3α) and Tyr216 (pGSK3β) with longer exposure (24 h) [1].