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Submit ReviewJQKD 82 dihydrochloride
Description: Selective inhibitor of lysine demethylase 5
Chemical Name: 2,4-Diisopropoxyphenyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for JQKD 82 dihydrochloride
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.
Licensing Information
Sold under license from Dana-Farber Cancer Institute
Technical Data for JQKD 82 dihydrochloride
| M. Wt | 573.56 |
| Formula | C27H40N4O5.2HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2863635-05-4 |
| InChI Key | LDSXMHKWRLCTDV-UHFFFAOYSA-N |
| Smiles | CCN(C(CNCC1=CC(C(OC2=C(C=C(C=C2)OC(C)C)OC(C)C)=O)=CC=N1)=O)CCN(C)C.Cl.Cl |
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.
Solubility Data for JQKD 82 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.68 | 50 |
Preparing Stock Solutions for JQKD 82 dihydrochloride
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 |
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Product Datasheets for JQKD 82 dihydrochloride
References for JQKD 82 dihydrochloride
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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Literature in this Area
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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Epigenetics Scientific Review
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.