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BioE-1115

CAS No. : 1268863-35-9

MCE 国际站：BioE-1115

产品活性：BioE-1115 是一种高度选择性和有效的 PAS 激酶 (PASK) 抑制剂，其 IC₅₀ 值约为 4 nM。BioE-1115 还是一种有效的酪蛋白激酶 2α (casein kinase 2α) 抑制剂，IC₅₀ 值约为 10 μM。

研究领域：Metabolic Enzyme/Protease  |  Cell Cycle/DNA Damage  |  Stem Cell/Wnt

作用靶点：Ser/Thr Protease  |  Casein Kinase

In Vitro: In the presence of BioE-1115, shows a dose-dependent loss of PASK phosphorylation, with an IC₅₀ of ~1μM in HEK293 cells.
At the concentrations above 10μM, BioE-1115 treatment shows a significant reduction in SREBP activity, without any observable effects on cell morphology or growth rate in HepG2 cells.

In Vivo: BioE-1115 (1-100 mg/kg; oral gavage; daily; for 7 days; male Sprague-Dawley rats) treatment shows a dose-dependent suppression of the expression of Gpat1, Fasn and all other SREBP-1c target genes analyzed. SREBP-1 maturation in liver is also suppressed in BioE-1115 treated rats at 10, 30 and 100 mg/kg doses. A calculated measure of insulin resistance, HOMA-IR, is decreased in a dose-dependent manner by BioE-1115 administration. Hepatic and serum TAG are decreased in a dose-dependent manner by BioE-1115 administration. BioE-1115 treatment causes a significant decrease in serum glucose. Both SREBP-1c and SREBP-1a mRNA are modestly decreased at the highest doses. Neither dose of BioE-1115 causes a significant change in either liver weight or body weight.

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