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BioE-1115

Catalog No.GC60078

BioE-1115 est un inhibiteur de la PAS kinase (PASK) hautement sélectif et puissant avec une IC50 d'environ 4 nM.

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BioE-1115 Chemical Structure

Cas No.: 1268863-35-9

Taille Prix Stock Qté
5mg
269,00 $US
En stock
10mg
445,00 $US
En stock
50mg
1 066,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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].

In the presence of BioE-1115, shows a dose-dependent loss of PASK phosphorylation, with an IC50 of ~1μM in HEK293 cells[1]. At the concentrations above 10μM, BioE-1115 treatment shows a significant reduction in SREBP activity, without any observable effects on cell morphology or growth rate in HepG2 cells[1].

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]

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

Chemical Properties

Cas No. 1268863-35-9 SDF
Canonical SMILES O=C(C1=CC=C2N=C(C3=CC=C(F)C=C3)C(N(C)C(C)C)=NC2=C1)O
Formula C19H18FN3O2 M.Wt 339.36
Solubility Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.9467 mL 14.7336 mL 29.4672 mL
5 mM 0.5893 mL 2.9467 mL 5.8934 mL
10 mM 0.2947 mL 1.4734 mL 2.9467 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

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