Aristolactam BIII
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models.
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- CAS No.: 53948-10-0
- Formula: C18H15NO4
- Molecular Weight:309.32
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B-cell | IC50 |
1.98 μM
Compound: 24
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Inhibition of LPS-induced BALB/c mouse B cell proliferation
Inhibition of LPS-induced BALB/c mouse B cell proliferation
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[PMID: 17081761] |
| HCT-15 | GI50 |
3.35 μM
Compound: 6
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Antiproliferative activity against multidrug resistant human HCT15/CLO2 cells by SRB assay
Antiproliferative activity against multidrug resistant human HCT15/CLO2 cells by SRB assay
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[PMID: 19394218] |
| HCT-15 | GI50 |
3.74 μM
Compound: 6
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Antiproliferative activity against human HCT15 cells by SRB assay
Antiproliferative activity against human HCT15 cells by SRB assay
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[PMID: 19394218] |
| MES-SA | GI50 |
2.7 μM
Compound: 6
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Antiproliferative activity against human MESSA cells by SRB assay
Antiproliferative activity against human MESSA cells by SRB assay
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[PMID: 19394218] |
| MES-SA/Dx5 | GI50 |
2.82 μM
Compound: 6
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Antiproliferative activity against multidrug resistant human MES-SA/Dx5 cells by SRB assay
Antiproliferative activity against multidrug resistant human MES-SA/Dx5 cells by SRB assay
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[PMID: 19394218] |
| T-cell | IC50 |
2.29 μM
Compound: 24
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Inhibition of ConA-induced BALB/c mouse T cell proliferation
Inhibition of ConA-induced BALB/c mouse T cell proliferation
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[PMID: 17081761] |
Chemical Information
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CAS No. 53948-10-0
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Molecular Weight 309.32
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Formula C18H15NO4
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SMILES
O=C1NC2=C3C1=CC(OC)=C(OC)C3=C4C(C=CC(OC)=C4)=C2
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Structure Classification
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Initial Source
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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)
Aristolactam BIII Related Classifications
HY-122989 Related Classifications
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