Toggle Nav
Close
  • Menu
  • Setting

TCS 2002

Catalog No.
B5486
GSK -3β inhibitor, potent
Grouped product items
SizePriceStock Qty
10mg
$307.00
Ship with 5-10 days
50mg
$1,213.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt338.38
Cas No.1005201-24-0
FormulaC18H14N2O3S
Solubility<33.84mg/ml in DMSO; <8.46mg/ml in ethanol
Chemical Name2-methyl-5-(3-(4-(methylsulfinyl)phenyl)benzofuran-5-yl)-1,3,4-oxadiazole
SDFDownload SDF
Canonical SMILESO=S(C)C1=CC=C(C=C1)C2=COC3=CC=C(C4=NN=C(C)O4)C=C23
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

TCS 2002