KDM5-C49
Based on 1 publication(s) in Google Scholar
KDM5-C49 (KDOAM-20) is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 can be used for the research of cancer.
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- CAS. Nr.: 1596348-16-1
- Formel: C15H24N4O3
- Molecular Weight:308.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) KDM5-C49
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Biologische Aktivität
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KDM5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
1 μM
Compound: 128
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay
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[PMID: 26710088] |
| MM1.S | EC50 |
>10 μM
Compound: 12
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Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
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[PMID: 34555614] |
| Sf9 | IC50 |
<0.1 μM
Compound: 128
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Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using biotinylated histone H3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using biotinylated histone H3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
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[PMID: 26710088] |
| Sf9 | IC50 |
<0.1 μM
Compound: 128
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Inhibition of recombinant human N-terminal FLAG-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
Inhibition of recombinant human N-terminal FLAG-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
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[PMID: 26710088] |
| Sf9 | IC50 |
>1 μM
Compound: 128
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Inhibition of human C-terminal FLAG-tagged KDM6B (1043 residues) expressed in baculovirus infected sf9 cells using H3K27me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
Inhibition of human C-terminal FLAG-tagged KDM6B (1043 residues) expressed in baculovirus infected sf9 cells using H3K27me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
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[PMID: 26710088] |
| Sf9 | IC50 |
>1 μM
Compound: 128
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Inhibition of recombinant KDM3B (842 to 1761 residues) (unknown origin) expressed in baculovirus infected sf9 cells using biotin-H3K9me as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
Inhibition of recombinant KDM3B (842 to 1761 residues) (unknown origin) expressed in baculovirus infected sf9 cells using biotin-H3K9me as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
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[PMID: 26710088] |
| Sf9 | IC50 |
0.1 μM
Compound: 128
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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 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
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[PMID: 26710088] |
| U2OS | IC50 |
1 μM
Compound: 128
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Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
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[PMID: 26710088] |
| U2OS | IC50 |
1 μM
Compound: 128
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Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
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[PMID: 26710088] |
KDM5-C49 display poor permeability. Convert the carboxylate group of KDM5-C49 into an ethyl ester, to get a cell-permeable prodrug (KDM5-C70)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1596348-16-1
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Molecular Weight 308.38
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Formel C15H24N4O3
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SMILES
O=C(C1=CC=NC(CNCC(N(CC)CCN(C)C)=O)=C1)O
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Synonyms
KDOAM-20
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Reinheit & Dokumentation
Verweise
[1]. Horton JR, et, al. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. Cell Chem Biol. 2016 Jul 21;23(7):769-781. [Content Brief]
[2]. Song YQ, et al. The role and prospect of lysine-specific demethylases in cancer chemoresistance. Med Res Rev. 2023 Apr 3. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
KDM5-C49 Related Classifications
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