LSD1-C76, LSD1 Inhibitor


Catalog No. size PriceQuantity
M66045-2D 10 mM in DMSO (0.678 mL) $159
M66045-2S 2mg solid $159
M66045-10S 10mg solid $636

Description

Product Information
Molecular Weight: 295.38
Formula: C19H21NO2
Purity: ≥98%
CAS#: 1235864-15-9
Solubility: DMSO up to 100 mM
Chemical Name:

(1R,2S)-N-(1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)ethyl)-2-phenylcyclopropanamine

Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

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.


 

 products are for research use only. Not for human use.

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