CAS NO: | 1005201-24-0 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Cas No. | 1005201-24-0 |
化学名 | 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 |
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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |