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Lysine Specific Demethylase 1-Selective Inhibitor

No.151(August 2013)
A2411
N-[(1S)-3-[3-(trans-2-Aminocyclopropyl)phenoxy]-1-(benzylcarbamoyl)propyl]benzamide Hydrochloride (= NCL-1•HCl)   (1)
Fig. 1

Fig. 1

NCL-1, developed by Suzuki, Mizukami, Miyata et al., inhibits lysine specific demethylase 1 (LSD1) which plays a key role in the regulation of gene expression by removing the methyl groups from methylated Lys4 of histone H3 (H3K4) (Fig. 1).1) LSD1 inhibitory activity of NCL-1 was more potent than that of a known LSD1 inhibitor, trans-2-phenylcyclopropylamine. NCL-1 showed H3K4-methylating activity and antiproliferative activity in cellular assays.
This product is a 1:1 mixture of two diastereomers (1R,2S) and (1S,2R) at the trans-cyclopropane ring.

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