1. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR Apoptosis
  2. Casein Kinase Akt Wnt Apoptosis
  3. Hematein

Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.

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Hematein Chemical Structure

Hematein Chemical Structure

CAS No. : 475-25-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
500 mg USD 55 In-stock
1 g USD 99 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Hematein

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Hematein is a oxidation product of hematoxylin acted as a dye[1]. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells[2].

IC50 & Target[2]

CKII

0.74 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HT-29 EC50
11.1 μM
Compound: Hematein
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HT-29 IC50
30.4 μM
Compound: Hematein
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
U2OS EC50
4.7 μM
Compound: Hematein
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
In Vitro

Hematein (10-100 μM; 14 days) inhibits cells growth in A427 lung cancer cells[1].
Hematein (50 and 100 μM; 48 hours) induces apoptosis in A427 lung cancer cells[1].
Hematein (50 and 100 μM; 48 hours) inhibits CK2-specific Akt phosphorylation[1].

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

Cell Viability Assay[1]

Cell Line: A427 (HTB-53) cell line
Concentration: 10-100 μM
Incubation Time: 14 days
Result: Inhibited cells growth.

Apoptosis Analysis[1]

Cell Line: A427 (HTB-53) cell line
Concentration: 50 and 100 μM
Incubation Time: 48 hours
Result: Induced apoptosis in A427 lung cancer cells.

Western Blot Analysis[1]

Cell Line: A427 (HTB-53) cell line
Concentration: 50 and 100 μM
Incubation Time: 48 hours
Result: Inhibited CK2-specific Akt phosphorylation.
In Vivo

Hematein (intraperitoneal injections; 50 mg/kg; twice a week for 6 weeks) inhibits tumor growth in A427 lung cancer cell xenografts[1].

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

Animal Model: Female athymic BALB/c nude mice (6-week-old) [1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injections; twice a week for 6 weeks
Result: Inhibited tumor growth in A427 lung cancer cell xenografts.
Molecular Weight

300.26

Formula

C16H12O6

CAS No.
Appearance

Solid

Color

Light brown to black

SMILES

O=C1C=C2CC3(C(C4=CC=C(C(O)=C4OC3)O)=C2C=C1O)O

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 : 100 mg/mL (333.04 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 3.3304 mL 16.6522 mL 33.3045 mL
5 mM 0.6661 mL 3.3304 mL 6.6609 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (8.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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(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, 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 3.3304 mL 16.6522 mL 33.3045 mL 83.2612 mL
5 mM 0.6661 mL 3.3304 mL 6.6609 mL 16.6522 mL
10 mM 0.3330 mL 1.6652 mL 3.3304 mL 8.3261 mL
15 mM 0.2220 mL 1.1101 mL 2.2203 mL 5.5507 mL
20 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1631 mL
25 mM 0.1332 mL 0.6661 mL 1.3322 mL 3.3304 mL
30 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7754 mL
40 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
50 mM 0.0666 mL 0.3330 mL 0.6661 mL 1.6652 mL
60 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 mL
80 mM 0.0416 mL 0.2082 mL 0.4163 mL 1.0408 mL
100 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8326 mL
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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.

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Product Name:
Hematein
Cat. No.:
HY-119751
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