产品说明书
(+)-JQ1
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同义名 : | - |
| CAS号 : | 1268524-70-4 | |
| 货号 : | A529842 | |
| 分子式 : | C23H25ClN4O2S | |
| 纯度 : | 98% | |
| 分子量 : | 456.99 | |
| MDL号 : | MFCD22683748 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 45 mg/mL(98.47 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear PO 0.5% CMC-Na 45 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | BRDs (bromodomains) of human proteome can recognize the relaxed chromatin segments and bind to the acetylated nucleosomes, transcription factors and co-activators. (+)-JQ1 is a potent and selective bromodomain inhibitor with IC50 values of 77nM, 33nM and >10uM for BRD4(1), BRD4(2) and CREBBP, respectively[1]. The (+)-JQ-1-specific inhibition of BRDs can affect the production of the targeted transcription factor-dependent protein, including NRF2-dependent HO-1, NADPH:quinone oxidoreductase-1 as well as GCLC, SOCS3, STAT5-mediated regulation of target genes, RUNX3, SIRT1, MYC and its downstream target genes, etc.[2]. JQ1 can induce the differentiation and growth arrest in NUT midline carcinoma. Treatment with (+)-JQ-1, 250nM for 48h, potently decreased the expression of both BRD4 target genes, RAD21 and RAN, in NMC cells. Treatment with JQ1, i.p., 50mg/kg for 18 days, can regress the tumor growth and prolong overall survival of NMC797 xenografted mice. In addition, (-)-JQ-1 is the negative control compound of (+)-JQ-1[1]. | ||
| 作用机制 | JQ1 can bind lysine acetylation binding site of BET bromodomains competitively with chromatin in a cellular environment.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 148I | Growth Inhibition Assay | 72 h | IC50=0.284±0.035 μM | 25944566 | |
| 148I | 0.25/0.5/1.0 μM | Apoptosis Assay | 24 h | increases levels of cleaved caspase-3 | 25944566 |
| 148I | 1 μM | Apoptosis Assay | 48 h | induces cell apoptosis significantly | 25944566 |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.94mL 2.19mL 1.09mL |
21.88mL 4.38mL 2.19mL |
| 参考文献 |
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