TCS 2002GSK -3β inhibitor, potent CAS# 1005201-24-0 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1005201-24-0 | SDF | Download SDF |
| PubChem ID | 24855958 | Appearance | Powder |
| Formula | C18H14N2O3S | M.Wt | 338.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 25 mM in ethanol | ||
| Chemical Name | 2-methyl-5-[3-(4-methylsulfinylphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazole | ||
| SMILES | CC1=NN=C(O1)C2=CC3=C(C=C2)OC=C3C4=CC=C(C=C4)S(=O)C | ||
| Standard InChIKey | RCKYSTKYIVULEK-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H14N2O3S/c1-11-19-20-18(23-11)13-5-8-17-15(9-13)16(10-22-17)12-3-6-14(7-4-12)24(2)21/h3-10H,1-2H3 | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent inhibitor of GSK-3β (IC50 = 35 nM). Oral adminstration inhibits cold water stress-induced tau hyperphosphorylation in the mouse brain. |
TCS 2002 Dilution Calculator
TCS 2002 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9553 mL | 14.7763 mL | 29.5526 mL | 59.1051 mL | 73.8814 mL |
| 5 mM | 0.5911 mL | 2.9553 mL | 5.9105 mL | 11.821 mL | 14.7763 mL |
| 10 mM | 0.2955 mL | 1.4776 mL | 2.9553 mL | 5.9105 mL | 7.3881 mL |
| 50 mM | 0.0591 mL | 0.2955 mL | 0.5911 mL | 1.1821 mL | 1.4776 mL |
| 100 mM | 0.0296 mL | 0.1478 mL | 0.2955 mL | 0.5911 mL | 0.7388 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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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.[Pubmed:19775160]
J Med Chem. 2009 Oct 22;52(20):6270-86.
Glycogen synthase kinase 3beta (GSK-3beta) inhibition is expected to be a promising therapeutic approach for treating Alzheimer's disease. Previously we reported a series of 1,3,4-oxadiazole derivatives as potent and highly selective GSK-3beta inhibitors, however, the representative compounds 1a,b showed poor pharmacokinetic profiles. Efforts were made to address this issue by reducing molecular weight and lipophilicity, leading to the identification of oxadiazole derivatives containing a sulfinyl group, (S)-9b and (S)-9c. These compounds exhibited not only highly selective and potent inhibitory activity against GSK-3beta but also showed good pharmacokinetic profiles including favorable BBB penetration. In addition, (S)-9b and (S)-9c given orally to mice significantly inhibited cold water stress-induced tau hyperphosphorylation in mouse brain.
