• 产品描述： 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

• 靶点： CK2α:10 μM (IC50);Serine/threoninkinase; CaseinKinase

• 体内研究：
  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. 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.

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

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.947 ml	14.733 ml	29.467 ml
  5 mM	0.589 ml	2.947 ml	5.893 ml
  10 mM	0.295 ml	1.473 ml	2.947 ml
  50 mM	0.059 ml	0.295 ml	0.589 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *