Name | BioE-1115 |
Description | 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)[1]. |
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[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 60 mg/mL (176.80 mM), Sonication is recommended.
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Keywords | Threonine proteases | BioE 1115 | BioE1115 | Ser/Thr Protease | Inhibitor | inhibit | BioE-1115 | Serine proteases | Serine endopeptidases | Casein Kinase |
Inhibitors Related | TBCA | Nafamostat mesylate | Ellagic acid | Emodin | LY-364947 | AS-252424 | Fasudil hydrochloride | Camostat mesylate | FOY 251 | Benzamidine hydrochloride | LY294002 | Cetraxate hydrochloride |
Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |