BioE-1115

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BioE-1115 是一种选择性、有效的丝氨酸-苏氨酸蛋白激酶 (PASK, IC50 = 4 nM) 抑制剂。

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 Vitro):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).(In Vivo):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.

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Animal Model:Male Sprague-Dawley rats (12 weeks of age; 129.4 ± 0.63 g) fed with high fructose diet Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg Administration:Oral gavage; daily; for 7 days Result: Treated with 10, 30 and 100 mg/kg, showed a dose-dependent suppression of the expression of Gpat1, Fasn and all other SREBP-1c target genes analyzed. Decreased hepatic expression of lipogenic SREBP-1c target genes, decreased serum triglycerides and partially reversed insulin resistance.

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Apoptosis

Serine/threonin kinase

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1268863-35-9

339.37

C19H18FN3O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (184.17 mM)

CC(C)N(C)c1nc2cc(ccc2nc1-c1ccc(F)cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years