JQKD82
JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form that retains the same biological activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2410512-38-6
- 分子式: C27H40N4O5
- 分子量:500.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
|
KDM5 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | EC50 |
0.42 μM
Compound: 48
|
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability
|
[PMID: 34555614] |
体外実験
JQKD82 (0.3 μM; 24 hours) causes an increase in the global H3K4me3 level of MM.1S cells[1].
JQKD82 (0.1-10 μM; day 1-day 5) inhibits the growth of MM.1S cells in a dose- and time-dependent manner. JQKD82 is potent at eliciting growth suppression in MM.1S cells (IC50=0.42 μM)[1].
JQKD82 (1 μM; 24 hours) induces G1 cell-cycle arrest by 48 hours in MM.1S and MOLP-8 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
JQKD82 displays an increase in H3K4me3 levels and results in a dramatic reduction of MYC immuno-staining in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice (bearing MOLP-8 TurboGFP-Luc cells)[1]
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Dosage:50 mg/kg, 75 mg/kg
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Administration:i.p.; twice a day for 3 weeks
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Result:Significantly reduced tumor burden.
化学情報
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CAS 番号 2410512-38-6
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分子量 500.63
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分子式 C27H40N4O5
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SMILES
O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OC2=CC=C(C=C2OC(C)C)OC(C)C
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別名
JADA82; PCK82
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)