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。

BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC 50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC 50 of ~10 μM.

Solid

CK2α 10 μM (IC50)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They

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Powder -20°C 3 years；4°C 2 years

[1]. Wu X, et al. PAS kinase drives lipogenesis through SREBP-1 maturation. Cell Rep. 2014 Jul 10;8(1):242-55.

In Vitro: DMSO : 62.5 mg/mL (184.17 mM; Need ultrasonic)配制储备液