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LSD1-C76 is the most potent and selective Lysine Specific Demethylase-1 (LSD1) inhibitor reported to date. It inhibits LSD1 with an IC₅₀ ~5 nM, but not monoamine oxidase proteins MAO-A and MAO-B (>5 µM). As LSD1 plays an important role in the epigenetic control of gene expression in normal development and cancer progression, LSD1-C76 serves as a very useful chemical probe to study the target biology.

How to Use:

• In vitro:  LSD1-C76 was used at 1 µM in vitro.
• In vivo: n/a

Reference:

• 1. GUIBOURT, Nathalie, et al. Preparation of phenylcyclopropylamine derivatives as LSD1 selective and LSD1/MAO-B dual inhibitors in treating or preventing cancer. PCT WO/2010/084160.
• 2. Shi Y, et al. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. (2004) Cell. 119(7):941-53.
• 3. Metzger E, et al. LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription. (2005) Nature. 437(7057):436-9.