JQKD 82 dihydrochloride

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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)
Datasheet
Citations
Reviews
Literature (3)

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)
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.

Select a batch to recalculate based on the batch molecular weight:
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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Citations for JQKD 82 dihydrochloride

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Literature in this Area

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