BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM .
BioE-1115 is a highly potent and selective inhibitor of PAS kinase (PASK), with an IC50 of approximately 4 nM. Additionally, BioE-1115 exhibits potent inhibition of casein kinase 2α, with an IC50 of around 10 μM [1].
体内研究
BioE-1115 treatment (administered orally via gavage at doses ranging from 1 to 100 mg/kg daily for 7 days in male Sprague-Dawley rats) results in a dose-dependent reduction in the expression of Gpat1, Fasn, and other analyzed SREBP-1 c target genes. Additionally, maturation of SREBP-1 in the liver is suppressed at doses of 10, 30, and 100 mg/kg. A calculated measure of insulin resistance, HOMA-IR, is decreased in a dose-dependent manner by BioE-1115 administration. Both hepatic and serum triglyceride levels decline dose-dependently with BioE-1115 treatment. Furthermore, BioE-1115 significantly lowers serum glucose levels. Although both SREBP-1c and SREBP-1a mRNA levels modestly decrease at higher doses, neither dose of BioE-1115 induces significant changes in liver or body weight [1].
体外研究
In the presence of BioE-1115, there is a dose-dependent reduction in PASK phosphorylation, with an IC50 of approximately 1 μM in HEK293 cells [1].
At concentrations exceeding 10 μM, treatment with BioE-1115 demonstrates a notable decrease in SREBP activity in HepG2 cells, with no observable impact on cell morphology or growth rate [1].
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