N19-0881
N19-0881 (Compound 33) is an orally active, potent and selective KDM5A/5B histone lysine demethylase inhibitor (IC50= 0.013 μM and 0.002 μM, respectively). N19-0881 is promising for research of epigenetically dysregulated tumors (e.g., breast cancer).
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- No. CAS: 1613410-75-5
- Fòrmula: C17H14ClN3O3
- Peso molecular:343.76
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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KDM5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
<0.1 μM
Compound: 101
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Inhibition of recombinant human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 substrate incubated for 30 mins by TR-FRET assay
Inhibition of recombinant human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 substrate incubated for 30 mins by TR-FRET assay
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[PMID: 26710088] |
| Sf9 | IC50 |
0.1 μM
Compound: 101
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Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 substrate incubated for 30 mins by alphascreen assay
Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 substrate incubated for 30 mins by alphascreen assay
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[PMID: 26710088] |
| ZR-75-1 | IC50 |
<0.1 μM
Compound: 101
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Inhibition of KDM5A in human ZR-75-1 cells assessed as reduction in H3K4me3 demethylation incubated for 72 hrs by fluorometric immunoassay
Inhibition of KDM5A in human ZR-75-1 cells assessed as reduction in H3K4me3 demethylation incubated for 72 hrs by fluorometric immunoassay
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[PMID: 26710088] |
Chemical Information
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No. CAS 1613410-75-5
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Peso molecular 343.76
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Fòrmula C17H14ClN3O3
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SMILES
O=C(C1=CC(N2N=CC=C2OCC3=CC=C(Cl)C=C3C)=NC=C1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
N19-0881 Related Classifications
HY-136682 Related Classifications
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