GSK3 Inhibitor XV

GSK3 inhibitor XV is a racemic mixture of (R)-GSK3 inhibitor XV and (S)-GSK3 inhibitor XV. (R)-GSK3 inhibitor XV inhibits glycogen synthase kinase (GSK) 3α and β (IC50s = 0.35 and 0.55 nM, respectively). It selectively inhibits GSK3α and β over a kinase panel including MSK1, RSK1, and TRKA (IC50s = 3,000, 8,000, and 350 nM, respectively), however, it also inhibits PIM-1 with an IC50 value of 35 nM. (R)-GSK3 inhibitor XV (1 μM) disrupts development of the anterior and posterior termini in zebrafish embryos. (S)-GSK3 inhibitor XV is less potent than the (R)-enantiomer, is selective for PIM-1 over GSK3 (IC50s = 3, 80, and 90 nM for PIM-1, GSK3α, and GSK3β, respectively), and has no effect on zebrafish embryonic development.