TWS119 is a glycogen synthase kinase-3β inhibitor with an IC50 of 30 nM. TWS119 induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs) at 400 nM.
|Cell lines||megakaryocytes (MKs)|
|Preparation method||To examine the inhibitory effects of p38MAPK, PI3K, and GSK-3β on MK differentiation and platelet production, hBMMNCs were cultured in MKLI media in the presence or absence (+/−) of each of the following inhibitors for 12 days: 5 µM SB202190 (AbMole, Houston, TX, USA) to inhibit p38MAPK; 10 µM LY294002 (AbMole, Houston, TX, USA) to inhibit PI3K; and 1 µM TWS119 (AbMole, Houston, TX, USA) to inhibit GSK-3β. To investigate the effect of GSK-3β inhibition on platelet production from mature MKs defined as CD41 (+)/CD42b (+)/propidium iodide (PI, Sigma) (−), as described later (flow cytometry analysis in the Methods), mature MKs were then cultured in MKLI media with TWS119 (+/−) for 6 days.|
|Concentrations||0, 0.17, 1, and 3 µM|
|Incubation time||12 days|
|Animal models||Permanent focal cerebral ischemia rats|
|Formulation||1 % DMSO|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
|Source||Exp Cell Res (2018). Figure 1. TWS119|
|Method||CFSE proliferation assay|
|Cell Lines||γδT cells|
|Incubation Time||72 h|
|Results||CFSE dilution assays showed that treatment of PBMCs with TWS119 (2 μM) could simulate γδT cells to divide robustly and with less cell apoptosis compared with the control group|
GSK-3β inhibitor TWS119 attenuates rtPA-induced hemorrhagic transformation and activates the Wnt/β-catenin signaling pathway after acute ischemic stroke in rats.
Wang W, et al. Mol Neurobiol. 2016 Dec;53(10):7028-7036. PMID: 26671619.
GSK-3β negatively regulates megakaryocyte differentiation and platelet production from primary human bone marrow cells in vitro.
Ono M, et al. Platelets. 2011;22(3):196-203. PMID: 21231855.
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