| Identification | Back Directory | [Name]
2-(4-fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid | [CAS]
1268863-35-9 | [Synonyms]
BioE1115
BIOE-1115
2-(4-fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid
6-Quinoxalinecarboxylic acid, 2-(4-fluorophenyl)-3-[methyl(1-methylethyl)amino]- | [Molecular Formula]
C19H18FN3O2 | [MDL Number]
MFCD31381032 | [MOL File]
1268863-35-9.mol | [Molecular Weight]
339.36 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
Cell permeable: yes''Primary Target
PASK | [in vivo]
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[1]. | Animal Model: | Male Sprague-Dawley rats (12 weeks of age; 129.4 ± 0.63 g) fed with high fructose diet[1] | | 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.
|
| [IC 50]
CK2α: 10 μM (IC50) | [References]
[1] Wu X, et al. PAS kinase drives lipogenesis through SREBP-1 maturation. Cell Rep. 2014 Jul 10;8(1):242-55. DOI:10.1016/j.celrep.2014.06.006 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
T&W GROUP
|
| Tel: |
021-61551611 13296011611 |
| Website: |
www.trustwe.com/ |
| Company Name: |
Struchem Co., Ltd.
|
| Tel: |
0512-63009836 18994340901 |
| Website: |
www.beidapharma.com |
|