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.
Front Pharmacol. 2023 Jun 29;14:1181319.
Liang-Ge-San: a classic traditional Chinese medicine formula, attenuates acute inflammation via targeting GSK3β
TWS119 purchased from AbMole
Aquaculture Reports. 2023 Dec;101784.
Squalene activates Wnt/β-Catenin signaling pathway to mediate NF-κB pathway to regulate inflammatory response and disease resistance in hybrid grouper
TWS119 purchased from AbMole
Biochim Biophys Acta Mol Cell Res. 2019 Mar;1866(3):486-503.
Protease-activated receptor 2 induces migration and promotes Slug-mediated epithelial-mesenchymal transition in lung adenocarcinoma cells.
TWS119 purchased from AbMole
Cell Experiment | |
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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 Experiment | |
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Animal models | Permanent focal cerebral ischemia rats |
Formulation | 1 % DMSO |
Dosages | 30 mg/kg |
Administration | intraperitoneal |
Molecular Weight | 318.33 |
Formula | C18H14N4O2 |
CAS Number | 601514-19-6 |
Solubility (25°C) | DMSO 38 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases. |
FRATtide
FRATtide is a peptide derived from the GSK-3 binding protein that inhibits the phosphorylation of Axin and β-catenin. |
ZDWX-25
ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. |
TC-G 24
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SAR502250
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. |
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