JQKD 82 dihydrochloride is cell-permeable, selective inhibitor of lysine demethylase 5 (KDM5). JQKD 82 does not show activity toward other KDMs; and it has selectivity for KDM5A over other KDM5 isoforms. JQKD 82 causes hypermethylation of H3K4me3, downregulation of MYC targets and RNAPII phosphorylation; it suppresses multiple myeloma cell (MM.1S) growth (IC50 = 0.42 μmol/L). JQKD 82-treated tumors display an increase in H3K4me3 levels and results in a reduction of MYC immuno-staining in NSG mice.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125576 |
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| Réf. fabricant | 18756886 |
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| Nom chimique ou matériau | 2,4-Diisopropoxyphenyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate dihydrochloride |
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| Quantité | 5 mg |
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| Cible | Histone Demethylase Inhibitors |
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| Formule moléculaire | C<sub>27</sub>H<sub>40</sub>N<sub>4</sub>O<sub>5</sub>0.2 HCl |
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| Pureté | 0.98 |
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