Cat. No.: HY-119751

Hematein

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

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

Purity: 59.09%
CAS No.: 475-25-2
Formula: C₁₆H₁₂O₆
Molecular Weight:300.26

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Hematein Chemical Structure

CAS No.: 475-25-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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)

All Casein Kinase Isoforms :

All Akt Isoforms :

All Wnt Isoforms :

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.

Chemical Information

CAS No. 475-25-2
Appearance Solid
Molecular Weight 300.26
Formula C₁₆H₁₂O₆
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

Publications (1)

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Journal Impact Factor

bioRxiv

2024 Jan 20.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3304 mL

16.6522 mL

33.3045 mL

5 mM

0.6661 mL

3.3304 mL

6.6609 mL

10 mM

0.3330 mL

1.6652 mL

3.3304 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

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In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Shirai, K., & Matsuoka, M. (1996). Structure and properties of hematein derivatives. Dyes and Pigments, 32(3), 159–169.

[2]. Hung MS, et al. Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograftmodel.Int J Oncol. 2013 Nov;43(5):1517-22. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Hematein

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

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Human Metabolite Library

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Cell Death Library

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Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

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Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Hematein

All Casein Kinase Isoforms

All Akt Isoforms

All Wnt Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Hematein Related Classifications

HY-119751 Related Classifications