2. PI3K/Akt/mTOR
  3. PI3K Akt
  4. Esculetin

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

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Esculetin Chemical Structure

Esculetin Chemical Structure

CAS No. : 305-01-1

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

Esculetin Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities[1].

IC50 & Target[1]

PI3K

 

In Vitro

Esculetin (40 μM, 24 h or 48 h) inhibits PDGF-BB-induced ASMC proliferation and migration[1].
Esculetin (40 μM, 1 h) inhibits PDGF-BB-induced ECM secretion and activation of PI3K/Akt pathway in ASMC cells[1].
Esculetin (100 μM, 36 h) induces pancreatic cancer cell (such as PANC-1 cells) apoptosis and loss of mitochondrial membrane potential by activation of caspases 3, 8 and 9[2].
Esculetin (100 μM, 0-12 h) binds to KEAP1 and inhibits its interaction with Nrf2 in pancreatic cancer cells (in PANC-1 cells)[2].

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

Esculetin Related Antibodies

Western Blot Analysis[2]

Cell Line: PANC-1 cells
Concentration: 100 μM
Incubation Time: 0-12 h
Result: Increased the amount of phosphorylated form of Nrf2.
Increased the levels of Nrf2 in nuclear.
Decreased NF-κB protein levels.
In Vivo

Esculetin (50 and 100 mg/kg/day, p.o., 7d) ameliorates skin lesion in Imiquimod (HY-B0180) (IMQ)-induced psoriatic mice[3].
Esculetin (10 or 30 mg/kg, i.p., three times per week for 28 days) inhibits tumor growth and metastasis via Axin2 suppression in an HCT116-implanted orthotopic mouse model[4].
Esculetin (oral gavage, 25 mg/kg for 35 days) inhibits acute restraint stress (ARS)-induced oxidative stress in mature adult mice by increasing antioxidant enzyme activities, the GSH/GSSG ratio, and cytochrome c oxidase activity in cortex[5].

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

Animal Model: Imiquimod (HY-B0180) (IMQ)-induced psoriatic mice[3]
Dosage: 50 and 100 mg/kg/day
Administration: p.o., 7d
Result: Ameliorated the skin lesion and reduced the PASI score.
Inhibited epidermal hyperplasia, and CD8 expression in the skin of psoriatic mice.
Molecular Weight

178.14

Formula

C9H6O4
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C1C=CC2=CC(O)=C(O)C=C2O1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (701.70 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 5.6136 mL 28.0678 mL 56.1356 mL
5 mM 1.1227 mL 5.6136 mL 11.2271 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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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 (11.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (11.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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

Purity: 99.59%

COA (249 KB) HNMR (227 KB) LCMS (282 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.6136 mL 28.0678 mL 56.1356 mL 140.3391 mL
5 mM 1.1227 mL 5.6136 mL 11.2271 mL 28.0678 mL
10 mM 0.5614 mL 2.8068 mL 5.6136 mL 14.0339 mL
15 mM 0.3742 mL 1.8712 mL 3.7424 mL 9.3559 mL
20 mM 0.2807 mL 1.4034 mL 2.8068 mL 7.0170 mL
25 mM 0.2245 mL 1.1227 mL 2.2454 mL 5.6136 mL
30 mM 0.1871 mL 0.9356 mL 1.8712 mL 4.6780 mL
40 mM 0.1403 mL 0.7017 mL 1.4034 mL 3.5085 mL
50 mM 0.1123 mL 0.5614 mL 1.1227 mL 2.8068 mL
60 mM 0.0936 mL 0.4678 mL 0.9356 mL 2.3390 mL
80 mM 0.0702 mL 0.3508 mL 0.7017 mL 1.7542 mL
100 mM 0.0561 mL 0.2807 mL 0.5614 mL 1.4034 mL
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Esculetin 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:

Esculetin305-01-1PI3KAktPhosphoinositide 3-kinasePKBProtein kinase BInhibitorinhibitorinhibit

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