| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 250mg | |||
| Other Sizes |
| Targets |
The primary target of Quinalizarin is casein kinase II (CK2), a ubiquitous and highly conserved serine/threonine protein kinase that phosphorylates a wide range of substrate proteins involved in cell proliferation, survival, and apoptosis. Quinalizarin acts as an ATP-competitive inhibitor, binding to the ATP-binding pocket of CK2. It inhibits CK2 with an IC50 of 110 nM and a Ki of approximately 50 nM. The compound demonstrates high selectivity for CK2, with IC50 values >1 μM against CK1 and 72 other kinases.
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| ln Vitro |
In vitro, Quinalizarin demonstrates potent and selective inhibition of CK2. Its activity is assessed in enzyme assays using recombinant CK2 and a peptide substrate, with the phosphorylation of the substrate measured in the presence of varying concentrations of the compound. The compound shows an IC50 of 110 nM for CK2 inhibition. Its selectivity is confirmed by profiling against a panel of other kinases. Quinalizarin also induces apoptosis in cancer cell lines. However, detailed cellular activity data are not extensively reported in the available literature.
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| ln Vivo |
In vivo data for Quinalizarin are not extensively reported in the available literature. As a potent and selective CK2 inhibitor, the compound has potential for in vivo applications in studying the role of CK2 in cancer and other diseases. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical.
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| Enzyme Assay |
In vitro enzyme assays for Quinalizarin typically involve measuring its inhibition of casein kinase II (CK2) activity. Recombinant CK2 enzyme is incubated with a peptide substrate (e.g., a synthetic peptide containing a CK2 phosphorylation site) and ATP in the presence of varying concentrations of Quinalizarin. The incorporation of phosphate into the substrate is measured, and the IC50 for inhibition is calculated. The compound's selectivity is assessed by profiling against a panel of other kinases.
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| Cell Assay |
Cellular assays for Quinalizarin are performed in various cancer cell lines to assess its effects on CK2 activity and cell viability. Cells are treated with Quinalizarin, and the phosphorylation of CK2 substrates is measured by Western blotting using phospho-specific antibodies. Cell viability is assessed using assays such as MTT or resazurin reduction. Apoptosis is measured by flow cytometry using Annexin V staining or by measuring caspase activity.
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| Animal Protocol |
In vivo animal studies with Quinalizarin are not extensively documented in the available literature. Based on its CK2 inhibitory activity, potential in vivo models could include xenograft models for cancer. In such studies, Quinalizarin would be administered orally or intraperitoneally, and tumor growth would be monitored. However, specific protocols are not detailed in the available sources.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Quinalizarin are not extensively reported. The compound is an anthraquinone derivative with a molecular weight that is not specified in the available literature. It is typically dissolved in DMSO for in vitro studies. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Quinalizarin has been reported to induce apoptosis in some cancer cells, indicating potential anticancer activity. However, comprehensive toxicology data for this compound are not extensively reported. As a CK2 inhibitor, it may have effects on cell proliferation and survival that could contribute to toxicity. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
Meng LQ, Wang Y, Luo YH, Piao XJ, Liu C, Wang Y, Zhang Y, Wang JR, Wang H, Xu WT, Liu Y, Wu YQ, Sun HN, Han YH, Jin MH, Shen GN, Fang NZ, Jin CH. Quinalizarin Induces Apoptosis through Reactive Oxygen Species (ROS)-Mediated Mitogen-Activated Protein Kinase (MAPK) and Signal Transducer and Activator of Transcription 3 (STAT3) Signaling Pathways in Colorectal Cancer Cells. Med Sci Monit. 2018 Jun 3;24:3710-3719. doi: 10.12659/MSM.907163. PubMed PMID: 29860266; PubMed Central PMCID: PMC6014151.
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| Additional Infomation |
Quinalizaline is a tetrahydroxyanthraquinone with four hydroxyl groups located at positions 1, 2, 5, and 8. It is an EC 2.7.11.1 (nonspecific serine/threonine protein kinase) inhibitor.
Quinalizarin is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying casein kinase II (CK2). Its high selectivity for CK2 makes it a valuable reagent for dissecting the specific functions of this kinase. The compound is used to study the role of CK2 in cell proliferation, survival, and apoptosis, as well as its potential as a therapeutic target in cancer and other diseases. |
| Molecular Formula |
C14H8O6
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|---|---|
| Molecular Weight |
272.21
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| Exact Mass |
272.032
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| CAS # |
81-61-8
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| PubChem CID |
5004
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| Appearance |
Orange to reddish brown solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
517.1±45.0 °C at 760 mmHg
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| Melting Point |
99 °C
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| Flash Point |
280.6±25.2 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.815
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| LogP |
5.18
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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 |
20
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VBHKTXLEJZIDJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H8O6/c15-6-3-4-7(16)11-10(6)12(18)5-1-2-8(17)13(19)9(5)14(11)20/h1-4,15-17,19H
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| Chemical Name |
1,2,5,8-Tetrahydroxyanthraquinone
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| Synonyms |
Alizarin Bordeaux BD Alizarinbordeaux Alizarine Bordeaux Alizarine
Bordeaux B C.I. 58500 C.I. Mordant Violet 26 Khinalizarin NSC
144046 NSC 4896 PHF 016 Quinalizarine Quinazarin
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6736 mL | 18.3682 mL | 36.7363 mL | |
| 5 mM | 0.7347 mL | 3.6736 mL | 7.3473 mL | |
| 10 mM | 0.3674 mL | 1.8368 mL | 3.6736 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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