TWS119GSK-3β inhibitor CAS# 601514-19-6 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 601514-19-6 | SDF | Download SDF |
| PubChem ID | 9549289 | Appearance | Powder |
| Formula | C18H14N4O2 | M.Wt | 318.33 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (157.07 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-[[6-(3-aminophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenol | ||
| SMILES | C1=CC(=CC(=C1)N)C2=CC3=C(N2)N=CN=C3OC4=CC=CC(=C4)O | ||
| Standard InChIKey | VPVLEBIVXZSOMQ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H14N4O2/c19-12-4-1-3-11(7-12)16-9-15-17(22-16)20-10-21-18(15)24-14-6-2-5-13(23)8-14/h1-10,23H,19H2,(H,20,21,22) | ||
| 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 | TWS119 is a GSK-3β inhibitor with an IC50 value of 30 nM. | |||||
| Targets | GSK-3β | |||||
| IC50 | 30 nM | |||||
TWS119 Dilution Calculator
TWS119 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1414 mL | 15.707 mL | 31.4139 mL | 62.8279 mL | 78.5349 mL |
| 5 mM | 0.6283 mL | 3.1414 mL | 6.2828 mL | 12.5656 mL | 15.707 mL |
| 10 mM | 0.3141 mL | 1.5707 mL | 3.1414 mL | 6.2828 mL | 7.8535 mL |
| 50 mM | 0.0628 mL | 0.3141 mL | 0.6283 mL | 1.2566 mL | 1.5707 mL |
| 100 mM | 0.0314 mL | 0.1571 mL | 0.3141 mL | 0.6283 mL | 0.7853 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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TWS119 is an inhibitor of glycogen synthase kinase-3β (GSK-3β) with IC50 value of 30nM [1].
TWS119 is screened out from a library of pyrrolopyrimidines as a molecule that selectively induces neuronal differentiation when using mouse P19 EC cells. TWS119 binds to GSK-3β tightly with a Kd value of 126nM and shows an inhibition with IC50 value of 30nM. The combination of TWS119 and GSK-3β modulates the activity of the complex and triggers downstream transcriptional events lead the neuronal induction. Besides that, TWS119 promotes neuronal differentiation of mESCs through another mechanism but not the canonical Wnt signaling pathway [1, 2].
References:
[1] Ding S, Wu T Y H, Brinker A, et al. Synthetic small molecules that control stem cell fate. Proceedings of the National Academy of Sciences, 2003, 100(13): 7632-7637.
[2] Wu T Y H, Ding S. Applying chemical tools to the discovery of novel regenerative medicine. Drug Discovery Today: Technologies, 2006, 3(3): 255-260.
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[Activation of Wnt/beta-catenin pathway in NK cells by glycogen synthase kinase-3beta inhibitor TWS119 promotes the expression of CD62L].[Pubmed:25575058]
Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2015 Jan;31(1):44-8.
OBJECTIVE: To investigate the effect of Wnt/beta-catenin pathway activation by glycogen synthase kinase-3beta inhibitor 4,6-disubstituted pyrrolopyrimidine (TWS119) on proliferation and phenotypic characteristics of human nature killer (NK) cells. METHODS: The peripheral blood mononuclear cells (PBMCs) were obtained from healthy volunteers and added to the complete medium containing recombinant human interleukin-2 (rhIL-2) and human AB serum to isolate NK cells from PBMCs. After co-cultured with 0-8.0 mumol/L TWS119 for 72 hours, growth curve and Wnt/beta-catenin activation of NK cells in each group were determined by CCK-8 and Western blotting. The CD107a and CD62L (L-selectin) expressions in the NK cells were detected using flow cytometry. RESULTS: NK cells were amplified to (61.76 +/- 3.74)% after human PBMCs were cultured for 10 days. The 0-2.0 mumol/L TWS119 could promote the growth of NK cells in a dose-dependent manner, and the proliferation rate gradually dropped when TWS119 was more than 2.0 mumol/L. 0-8.0 mumol/L TWS119 could activate Wnt/beta-catenin pathway and up-regulate the expression of CD62L in a dose-dependent manner, but it decreased the expression of CD107a. CONCLUSION: Human NK cells isolated from peripheral blood treated with TWS119 gave rise to early mature CD62L(+) NK cells.
GSK-3beta inhibitor TWS119 attenuates rtPA-induced hemorrhagic transformation and activates the Wnt/beta-catenin signaling pathway after acute ischemic stroke in rats.[Pubmed:26671619]
Mol Neurobiol. 2016 Dec;53(10):7028-7036.
Hemorrhagic transformation (HT) is a devastating complication for patients with acute ischemic stroke who are treated with tissue plasminogen activator (tPA). It is associated with high morbidity and mortality, but no effective treatments are currently available to reduce HT risk. Therefore, methods to prevent HT are urgently needed. In this study, we used TWS119, an inhibitor of glycogen synthase kinase 3beta (GSK-3beta), to evaluate the role of the Wnt/beta-catenin signaling pathway in recombinant tPA (rtPA)-induced HT. Sprague-Dawley rats were subjected to a middle cerebral artery occlusion (MCAO) model of ischemic stroke and then were administered rtPA, rtPA combined with TWS119, or vehicle at 4 h. The animals were sacrificed 24 h after infarct induction. Rats treated with rtPA showed evident HT, had more severe neurologic deficit, brain edema, and blood-brain barrier breakdown, and had larger infarction volume than did the vehicle group. Rats treated with TWS119 had significantly improved outcomes compared with those of rats treated with rtPA alone. In addition, Western blot analysis showed that TWS119 increased the protein expression of beta-catenin, claudin-3, and ZO-1 while suppressing the expression of GSK-3beta. These results suggest that TWS119 reduces rtPA-induced HT and attenuates blood-brain barrier disruption, possibly through activation of the Wnt/beta-catenin signaling pathway. This study provides a potential therapeutic strategy to prevent tPA-induced HT after acute ischemic stroke.
