ChemicalBook CAS DataBase List 1268863-35-9

1268863-35-9

Name	2-(4-fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid
CAS	1268863-35-9
Molecular Formula	C19H18FN3O2
MDL Number	MFCD31381032
Molecular Weight	339.36
MOL File	1268863-35-9.mol

Chemical Properties

storage temp.	2-8°C
solubility	DMSO: 50mg/mL
form	Solid
color	Light yellow to yellow

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338
WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

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

Spectrum Detail

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