CeMMEC1 HCl

製品コードS8328 バッチS832801

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C19H17ClN2O4

分子量 372.8 CAS No. 2095432-53-2
Solubility (25°C)* 体外 DMSO 23 mg/mL (61.69 mM)
Ethanol 1 mg/mL (2.68 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 CeMMEC1は、TAF1の第二ブロモドメインを阻害する(IC50=0.9 μM)N-メチルイソキノリノン誘導体です。
in vitro CeMMEC1 only bound BRD4 very weakly but it shows high affinity for the bromodomains of CREBBP, EP300, BRD9 and the second bromodomain of TAF1.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 REDS3 cells
濃度 10 μM
反応時間 24 h
実験の流れ

REDS3 cells were treated with 10 μM of every compound, and live-cell imaging pictures were taken to assess their ability to induce RFP expression 24 h later. From this primary screening 1,286 small molecules were selected as hits and rescreened in the follow-up part, in which REDS3 and WT KBM7 cells were treated in three-point dose response in order to exclude autofluorescent or toxic compounds. 80 small molecules were selected as hits and used to treat WT KBM7 cells and REDS3 cells in eight-point dose (twofold dilution, starting from 100 μM) response and three-point time course (24 h, 48 h and 72 h) to carefully select the best true hits (time- and dose-dependent RFP expression/no autofluorescence). UPLC-MS analysis was done to confirm purity and the correct mass of the small molecules selected; finally, 22 small molecules fulfilled the criteria as screening hits.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27159579/

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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