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Description: BioE-1115 (BioE 1115) is a novel, potent and highly selective PAS kinase (PASK) inhibitor with an IC50 of ~4 nM, it is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM. It is a dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α).
| ln Vitro |
With an IC50 of approximately 1 μM in HEK293 cells, a dose that is thought to cause a loss of PASK phosphorylation was demonstrated in the presence of BioE-1115 [1]. When BioE-1115 was applied at a dose of 10 μM, HepG2 cell growth rate and cell shape did not exhibit any discernible changes, but SREBP activity was significantly reduced [1].
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| ln Vivo |
Doses of Gpat1, Fasn, and all other SREBP-1c target gene expression examined in BioE-1115 (1-100 mg/kg; borderline gavage; daily; for 7 days; cosmetic Sprague-Dawley construct) were found to be dose regulators. SREBP-1 saturation in Manhattan was also inhibited at doses of 10, 30, and 100 mg/kg treated with 1115. BioE-1115 was applied in a dose-dependent manner to decrease HOMA-IR, a computed marker of insulin resistance. By using BioE-1115, liver and serum TAG were decreased in a dose-dependent manner. Serum blood glucose levels significantly dropped after receiving BioE-1115 therapy. At the highest dose, the mRNA for SREBP-1c and SREBP-1a fell consistently.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (12 weeks old; 129.4 ± 0.63 g) fed a high-fructose diet [1]
Doses: 1 mg of BioE-1115 did not cause significant changes in body weight or weight [1]. /kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg Route of Administration: po (oral gavage); daily; 7-day Experimental Results: Treatment with 10, 30 and 100 mg/kg, shown Dose-dependent inhibition of Gpat1, Fasn, and all other SREBP-1c target gene expression analyzed. Hepatic expression of lipogenic SREBP-1c target genes was diminished, serum triglycerides were diminished and insulin resistance was partially reversed. |
| References |
| Molecular Formula |
C19H18FN3O2
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|---|---|
| Molecular Weight |
339.363527774811
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| Exact Mass |
339.138
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| CAS # |
1268863-35-9
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| Related CAS # |
1268863-35-9
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| PubChem CID |
50922674
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
468
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(=CC=1)C1C(=NC2C=C(C(=O)O)C=CC=2N=1)N(C)C(C)C
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| InChi Key |
JKKRYYTVQXUOKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18FN3O2/c1-11(2)23(3)18-17(12-4-7-14(20)8-5-12)21-15-9-6-13(19(24)25)10-16(15)22-18/h4-11H,1-3H3,(H,24,25)
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| Chemical Name |
2-(4-fluorophenyl)-3-[methyl(propan-2-yl)amino]quinoxaline-6-carboxylic acid
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| Synonyms |
BioE-1115BioE 1115BioE1115
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~184.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.13 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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