CeMMEC1 HCl

製品コードS8328 バッチS832801

化学情報

	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
* <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 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM).
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^[1].

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

[1] Sdelci S, et al. Nat Chem Biol. 2016, 12(7):504-10.

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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