2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Stem Cell/Wnt
  3. Ser/Thr Protease Casein Kinase
  4. BioE-1115

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.

For research use only. We do not sell to patients.

BioE-1115 Chemical Structure

BioE-1115 Chemical Structure

CAS No. : 1268863-35-9

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10 mM * 1 mL in DMSO
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10 mg USD 90 In-stock
50 mg USD 230 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BioE-1115 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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].

IC50 & Target[1]

CK2α

10 μM (IC50)

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BioE-1115 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

339.36

Formula

C19H18FN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C2N=C(C3=CC=C(F)C=C3)C(N(C)C(C)C)=NC2=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (184.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.08 mg/mL (6.13 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9467 mL 14.7336 mL 29.4672 mL 73.6681 mL
5 mM 0.5893 mL 2.9467 mL 5.8934 mL 14.7336 mL
10 mM 0.2947 mL 1.4734 mL 2.9467 mL 7.3668 mL
15 mM 0.1964 mL 0.9822 mL 1.9645 mL 4.9112 mL
20 mM 0.1473 mL 0.7367 mL 1.4734 mL 3.6834 mL
25 mM 0.1179 mL 0.5893 mL 1.1787 mL 2.9467 mL
30 mM 0.0982 mL 0.4911 mL 0.9822 mL 2.4556 mL
40 mM 0.0737 mL 0.3683 mL 0.7367 mL 1.8417 mL
50 mM 0.0589 mL 0.2947 mL 0.5893 mL 1.4734 mL
60 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2278 mL
80 mM 0.0368 mL 0.1842 mL 0.3683 mL 0.9209 mL
100 mM 0.0295 mL 0.1473 mL 0.2947 mL 0.7367 mL
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BioE-1115 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BioE-11151268863-35-9BioE1115BioE 1115Ser/Thr ProteaseCasein KinaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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