| Size | Price | Stock | Qty |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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| Other Sizes |
| Targets |
Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. It inhibits Akt/PKB Ser129 phosphorylation and the Wnt/TCF pathway. By inhibiting casein kinase II, Hematein modulates phosphorylation of downstream targets such as Akt. Its mechanism of action involves allosteric inhibition of casein kinase II, leading to reduced Akt phosphorylation and Wnt/TCF pathway activity, ultimately increasing apoptosis in cancer cells.
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| ln Vitro |
In A427 lung cancer cells, hematein (10–100 μM; 14 days) suppresses cell growth[1]. Hematein (50 and 100 μM; 48 hours) causes A427 lung cancer cells to undergo apoptosis[1]. 48 hours) suppresses Akt phosphorylation that is unique to CK2[1].
In vitro, Hematein (10-100 μM; 14 days) suppresses cell growth in A427 lung cancer cells. Hematein (50 and 100 μM; 48 hours) causes A427 lung cancer cells to undergo apoptosis and inhibits CK2-specific Akt phosphorylation. Its in vitro activity is characterized by potent inhibition of casein kinase II, suppression of Akt phosphorylation, and induction of apoptosis in lung cancer cells. |
| ln Vivo |
In A427 lung cancer cell xenografts, hematein (intraperitoneal injections; 50 mg/kg; twice weekly for 6 weeks) suppresses tumor growth[1].
In vivo, Hematein (intraperitoneal injections; 50 mg/kg; twice weekly for 6 weeks) suppresses tumor growth in A427 lung cancer cell xenografts in female athymic BALB/c nude mice. Its in vivo efficacy is attributed to its ability to inhibit casein kinase II, suppress Akt phosphorylation, and induce apoptosis in cancer cells. These findings demonstrate its potential as an anticancer agent in preclinical models. |
| Enzyme Assay |
In vitro enzyme assays for Hematein typically involve measuring the inhibition of casein kinase II activity. The compound is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. These assays confirm its mechanism of action as a casein kinase II inhibitor. Its effects on Akt phosphorylation can also be assessed using kinase assays or Western blotting.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: A427 (HTB-53) cell line Tested Concentrations: 10-100 μM Incubation Duration: 14 days Experimental Results: Inhibited cells growth. Apoptosis Analysis[1] Cell Types: A427 (HTB-53) cell line Tested Concentrations: 50 and 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced apoptosis in A427 lung cancer cells. Western Blot Analysis[1] Cell Types: A427 (HTB-53) cell line Tested Concentrations: 50 and 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited CK2-specific Akt phosphorylation. In vitro cellular assays for Hematein typically involve treating cancer cell lines such as A427 lung cancer cells with the compound and measuring cell viability, proliferation, and apoptosis. Hematein (10-100 μM; 14 days) suppresses cell growth, and (50 and 100 μM; 48 hours) induces apoptosis and inhibits CK2-specific Akt phosphorylation. These cell-based studies demonstrate its anticancer activity and its mechanism of action as a casein kinase II inhibitor. |
| Animal Protocol |
Animal/Disease Models: Female athymic BALB/c nude mice (6weeks old) [1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip)injections; twice a week for 6 weeks Experimental Results: Inhibited tumor growth in A427 lung cancer cell xenografts. In vivo animal models for Hematein involve A427 lung cancer cell xenografts in female athymic BALB/c nude mice. Hematein is administered via intraperitoneal injections at 50 mg/kg twice weekly for 6 weeks. Tumor growth inhibition is assessed. These studies provide evidence for its in vivo anticancer efficacy. Doses and administration routes are optimized based on the specific model and experimental endpoints. |
| ADME/Pharmacokinetics |
Hematein has a molecular formula of C16H12O6 and a molecular weight of 300.26. Its CAS number is 475-25-2. The compound is an organic heterotetracyclic compound with the chemical formula -6a,7-dihydrobenzo[b]indeno[1,2-d]pyran-9-one, containing four hydroxyl substituents at positions 3, 4, 6a, and 10. It is a histological dye. Hematein is an oxidation product of hematoxylin.
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| Toxicity/Toxicokinetics |
Hematein is a casein kinase II inhibitor with anticancer activity. As with any kinase inhibitor, potential toxicity may include off-target effects on other kinases and disruption of normal cellular signaling. The compound's safety profile should be evaluated in preclinical toxicology studies. Hematein is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying casein kinase II biology and cancer.
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| References | |
| Additional Infomation |
Hematein is an organic heterotetracyclic compound with the chemical formula -6a,7-dihydrobenzo[b]indeno[1,2-d]pyran-9-one, containing four hydroxyl substituents at positions 3, 4, 6a, and 10. It is a histological dye. Hematein belongs to the classes of enols, organic heterotetracyclic compounds, phenols, quinone methanes, and tertiary alcohols.
Hematein (CAS# 475-25-2) is an oxidized analogue of Hematoxylin used as a dye. It acts as an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein has anticancer activity by inhibiting Akt/PKB Ser129 phosphorylation and the Wnt/TCF pathway, and increasing cancer cell apoptosis. It suppresses tumor growth in A427 lung cancer cell xenografts. The compound is for research use only and not for human therapeutic use. |
| Molecular Formula |
C16H12O6
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| Molecular Weight |
300.26288
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| Exact Mass |
300.063
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| CAS # |
475-25-2
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| Related CAS # |
475-25-2 (Hematein);517-28-2 (Hematoxylin);
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| PubChem CID |
135403802
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| Appearance |
Light brown to black solid powder
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| Density |
1.77g/cm3
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| Boiling Point |
753.1ºC at 760mmHg
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| Melting Point |
180ºC
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| Flash Point |
289ºC
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| Vapour Pressure |
1.32E-17mmHg at 25°C
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| Index of Refraction |
1.765
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| LogP |
1.329
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
22
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| Complexity |
645
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HNNSUZPWERIYIL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12O6/c17-10-2-1-8-13-9-4-12(19)11(18)3-7(9)5-16(13,21)6-22-15(8)14(10)20/h1-4,18-21H,5-6H2
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| Chemical Name |
4,6a,9,10-tetrahydroxy-6,7-dihydroindeno[2,1-c]chromen-3-one
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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 : ~100 mg/mL (~333.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3330 mL | 1.6652 mL | 3.3304 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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