GSK2879552, Lysine Demethylase inhibitor (TBI4020)

Description

Product Details

Formal Name: 4-[[4-[[[(1R,2S)-2-Phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]benzoic acid dihydrochloride

Molecular Formula: C₂₃H₂₈N₂O₂ ·2HCl

Formula Weight: 437.40

CAS Number: 1401966-69-5

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml) and in Water (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Lysine Demethylase inhibitor

Functions

GSK289552 is potent, selective, and irreversible inhibitor of Lysine Demethylase 1 (LSD1) via covalent modification of the LSD1 cofactor FAD (Ki = 1.7 µM). It is selective for LSD1 over the closely related LSD2, MAO-A, MAO-B, and the FAD dependent enzymes D-amino acid oxidase and glutathione reductase. Tested against a panel of 165 cancer cell lines, GSK2879552 inhibited the proliferation of 9 small cell lung carcinoma lines and 20 AML cell lines.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml) and in Water (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.