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TCS 2002
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TCS 2002图片
CAS NO:1005201-24-0
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
TCS 2002 (Compound 9b) 是一种高选择性、口服生物利用度和有效的 GSK-3β;抑制剂,IC50 为 35 nM。
Cas No.1005201-24-0
化学名2-methyl-5-(3-(4-(methylsulfinyl)phenyl)benzofuran-5-yl)-1,3,4-oxadiazole
Canonical SMILESO=S(C)C1=CC=C(C=C1)C2=COC3=CC=C(C4=NN=C(C)O4)C=C23
分子式C18H14N2O3S
分子量338.38
溶解度<33.84mg/ml in DMSO;<8.46mg/ml in ethanol
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.