LSD1-C76, CAS No. 1235864-15-9, 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.

Product information

CAS Number: 1235864-15-9

Molecular Weight: 295.38

Formula: C19H21NO2

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

Smiles: CC(N[C@@H]1C[C@H]1C1C=CC=CC=1)C1=CC2OCCOC=2C=C1

InChiKey: PAXGPAVOMLKKDQ-ZMKYACIDSA-N

InChi: InChI=1S/C19H21NO2/c1-13(15-7-8-18-19(11-15)22-10-9-21-18)20-17-12-16(17)14-5-3-2-4-6-14/h2-8,11,13,16-17,20H,9-10,12H2,1H3/t13?,16-,17+/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

LSD1-C76 was used at 1 µM in vitro.

References:

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.