An orally bioavailable and blood-brain-barrier permeable oxadiazolo-benzofuranylphenylsulfoxide compound that acts as a potent, reversible and ATP-competitive inhibitor of GSK-3b (IC50=35nM, 34 and 140nM for racemic, (S)-9b eutomer and (R)-9b distomer). The (S)-9b eutomer displays excellent selectivity (IC50 > 10uM) over Cdk1/2/5, Chk1, p38a, JNK1, MEKK1, IKKb, PKCth, CK1d, EGFR, ErbB2, Src, Lck, IR, Tie2, c-Kit, c-Met, VEGFR2, FGFR3 and PDGFRa/b, and lowers tau phosphorylation at GSK-3b-Thr205 in a CWS (cold water stress) mouse model (3mg/kg, p.o.)
Formula:C18H14N2O3S
Solubility:DMSO or EtOH
Molecular Weight:338.4
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
