| Description |
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases[1].
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| Related Catalog |
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| Target |
GSK-3β:17.1 nM (IC50)
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| In Vitro |
TC-G 24 (Compound 24) binds to the ATP binding site of GSK-3β[1]. TC-G 24 (1 µM, 4 h) blocks the FBW7α-mediated degradation of TPP1 in human embryonic kidney (HEK) 293T cells[2]. Western Blot Analysis[2] Cell Line: 293T cells Concentration: 1 μM Incubation Time: 4 h Result: Blocked the FBW7α-mediated degradation of TPP1
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| In Vivo |
TC-G 24 (Compound 24) (0-15 mg/kg; i.p.; once) significantly raises liver glycogen content in a dose-dependent manner without obvious toxicity and can cross the BBB[1]. Animal Model: Six-week-old male C57BL/6N mice with weights averaging 22 g[1] Dosage: 1, 5, and 15 mg/kg Administration: Intraperitoneal injection, once Result: Significantly raised liver glycogen content in a dose-dependent manner without obvious toxicity. Was detected in the brain at concentrations higher than in plasma for all three tested doses (38 ± 6, 113 ± 54 and 286 ± 58 ng/g brain tissue at 1, 5 and 15 mg/kg, respectively).
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| References |
[1]. Khanfar MA, et al. Discovery of novel GSK-3β inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening. J Med Chem. 2010 Dec 23;53(24):8534-45. [2]. Lihui Wang, et al. FBW7 Mediates Senescence and Pulmonary Fibrosis through Telomere Uncapping. Cell Metab. 2020 Nov 3;32(5):860-877.e9.
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