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Submit ReviewJQKD 82 dihydrochloride
说明： Selective inhibitor of lysine demethylase 5
化学名： 2,4-Diisopropoxyphenyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate dihydrochloride
纯度： ≥98% (HPLC)
生物活性 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.
许可信息
Sold under license from Dana-Farber Cancer Institute
技术数据 for JQKD 82 dihydrochloride
| 分子量 | 573.56 |
| 公式 | C27H40N4O5.2HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for JQKD 82 dihydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 28.68 | 50 |
制备储备液 for JQKD 82 dihydrochloride
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for JQKD 82 dihydrochloride
参考文献 for JQKD 82 dihydrochloride
参考文献是支持产品生物活性的出版物。
Ohguchi et al (2021) Lysine demethylase 5A is required for MYC driven transcription in multiple myeloma. Blood Cancer Discov. 2 370 PMID: 34258103
If you know of a relevant reference for JQKD 82 dihydrochloride, please let us know.
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.