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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.
Sold under license from Dana-Farber Cancer Institute
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 573.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||3.49 mL||17.43 mL||34.87 mL|
|2.5 mM||0.7 mL||3.49 mL||6.97 mL|
|5 mM||0.35 mL||1.74 mL||3.49 mL|
|25 mM||0.07 mL||0.35 mL||0.7 mL|
References are publications that support the biological activity of the product.
Ohguchi et al (2021) Lysine demethylase 5A is required for MYC driven transcription in multiple myeloma. Blood Cancer Discov. 2 370 PMID: 34258103
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including: