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TCS 2002 GSK -3β inhibitor, potent

Catalog No.B5486
Size Price Stock Qty
10mg
$279.00
In stock
50mg
$1,133.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

TCS 2002

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Chemical Properties

Cas No. 1005201-24-0 SDF Download SDF
Chemical Name 2-methyl-5-(3-(4-(methylsulfinyl)phenyl)benzofuran-5-yl)-1,3,4-oxadiazole
Canonical SMILES O=S(C)C1=CC=C(C=C1)C2=COC3=CC=C(C4=NN=C(C)O4)C=C23
Formula C18H14N2O3S M.Wt 338.38
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance White solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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].

Reference:
[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.