2-Methyl-5-[3-[4-(methylsulfinyl)phenyl]-5-benzofuranyl]-1,3,4-oxadiazole

TCS 2002 is a Wnt/β-catenin signaling modulator, which is associated with diseases such as cancer and Alzheimer’s diasease.

tcs 2002 is a potent inhibitor of gsk-3β with ic50 value of 35 nm [1].glycogen synthase kinase 3 (gsk-3) is a serine/threonine protein kinase and functions by phosphorylating a serine or threonine residue on its target protein. gsk3β plays an important role in neuronal cell development, energy metabolism and body pattern formation.tcs 2002 is a potent gsk -3β inhibitor with ic50 value of 35 nm. (s) -tcs 2002 and (r) -tcs 2002 inhibited gsk-3β with ic50 values of 34 and 140 nm, respectively. tcs 2002 exhibited good bioavailability (f=40%) and solubility (38 μg/ml). (s) -tcs 2002 showed no inhibitory activity against 12 tyrosine kinases and 10 serine/threonine kinases up to 10 μm, indicating that (s) -tcs 2002 was a highly selective gsk -3β inhibitor [1].in mice, cold water stress (cws) induced tau hyperphosphorylation at several gsk -3β directed sites such as s199, thr205, thr231 and ser396. (s) -tcs 2002 significantly inhibited tau phosphorylation by 35% [1].

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[1]. saitoh m, kunitomo j, kimura e, et al. 2-{3-[4-(alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability. j med chem, 2009, 52(20): 6270-6286.