BioE-1115 是一种特异性和有效的丝氨酸-苏氨酸蛋白激酶抑制剂 (PASK, IC50 = 4 nM)。 BioE-1115 是一种有效的酪蛋白激酶 2α 抑制剂 (IC50 = 10 μM)。

BioE-1115 is a selective and potent inhibitor of serine-threonine protein kinase (PASK, IC50 = 4 nM). BioE-1115 is a potent inhibitor of CK2α (IC50 = 10 μM).

In HepG2 cells, BioE-1115 (>10μM) treatment shows a significant reduction in SREBP activity, without any observable effects on cell morphology or growth rate. In HEK293 cells, BioE-1115 shows a dose-dependent loss of PASK phosphorylation (IC50 =1μM)[1].

In male Sprague-Dawley rats, BioE-1115 (10, 30 and 100 mg/kg) treatment shows a dose-dependent suppression of the expression of Gpat1, Fasn, and all other SREBP-1c target genes analyzed. SREBP-1 maturation in the liver is also suppressed in BioE-1115 treated rats. 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[1].

1268863-35-9

C19H18FN3O2

339.36

DMSO:60 mg/mL (176.80 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years