MS049

製品コードS8147 バッチS814701

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	C₁₅H₂₆Cl₂N₂O
	分子量	321.29	CAS No.	2095432-59-8
Solubility (25°C)*	体外	DMSO	56 mg/mL (174.29 mM)
		Water	56 mg/mL (174.29 mM)
		Ethanol	50 mg/mL (155.62 mM)
* <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	MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
in vitro	MS049 does not inhibit any of the methyltransferases at 50 μM or demethylases at 10 μM and does not display appreciable binding to any of the methyllysine/methylarginine reader proteins using the DSF assay at 200 μM. MS049 demonstrated excellent selectivity over a broad range of epigenetic and nonepigenetic targets. In cellular assays, MS049 potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells^[1].

製品説明

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.

in vitro

MS049 does not inhibit any of the methyltransferases at 50 μM or demethylases at 10 μM and does not display appreciable binding to any of the methyllysine/methylarginine reader proteins using the DSF assay at 200 μM. MS049 demonstrated excellent selectivity over a broad range of epigenetic and nonepigenetic targets. In cellular assays, MS049 potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK293 cells
	濃度	0, 1, 10, and 50 μM
	反応時間	96 h
	実験の流れ	HEK293 cells grown in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL) were seeded on 96-well plates at density 3000/well and treated with compounds at 0, 1, 10, and 50 μM concentrations for 96 h. The confluency was measured using IncuCyte ZOOM live cell imaging device and analyzed with IncuCyte ZOOM software based on phase contrast images.

参考

[1] Shen Y, et al. J Med Chem. 2016, 59(19):9124-9139.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Hypoxia stimulates SUMOylation-dependent stabilization of KDM5B [ Research Square, 2021, 10.21203/rs.3.rs-620216/v1]	PubMed: None
Arginine Methylation-Dependent LSD1 Stability Promotes Invasion and Metastasis of Breast Cancer [ EMBO Rep, 2020, 21(2):e48597]	PubMed: 31833203

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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