Echiguanine B
Echiguanine B is a phosphatidylinositol-4-kinase (PI4K) inhibitor with an IC50 of 0.11 μg/mL against human targets. Echiguanine B inhibits phosphatidylinositol-4-kinase activity in the cell membranes of epithelial cancer cells. Echiguanine B can be used in cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 137319-26-7
- Formula: C10H14N6O2
- Molecular Weight:250.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PI4K 0.11 μg/mL (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.18 μg/mL
Compound: 2 (echiguanine B)
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Inhibition of Phosphatidylinositol 4-kinase of human epidermoid carcinoma A431 cells
Inhibition of Phosphatidylinositol 4-kinase of human epidermoid carcinoma A431 cells
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10.1016/S0960-894X(97)00122-4 |
| A-431 | IC50 |
0.11 μg/mL
Compound: 2, Echiguanine B
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Inhibition of phosphatidylinositol 4-kinase in human A431 cell membrane by liquid scintillation counting
Inhibition of phosphatidylinositol 4-kinase in human A431 cell membrane by liquid scintillation counting
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[PMID: 1666120] |
In Vitro
Echiguanine B (20 min at 20°C) inhibits phosphatidylinositol-4-kinase from A431 cell membranes with an IC50 of 0.11 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 137319-26-7
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Molecular Weight 250.26
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Formula C10H14N6O2
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SMILES
O=C1N=C(NC2=C1C(C(NCCCN)=O)=CN2)N
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Structure Classification
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Initial Source
STREPTOMYCES SP.
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Echiguanine B Related Classifications
HY-N19772 Related Classifications
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