GSK-LSD1 (hydrochloride) is a potent, irreversible, and mechanism-based inhibitor of LSD1.

In vitro: GSK-LSD1 inhibited the activity of LSD1 (IC50: 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes, such as LSD2, MAO-A, and MAO-B. GSK-LSD1 inhibited cell proliferation by inducing gene expression changes in various cancer cell lines, the EC50s were< 5 nM [1].

In vivo: In mice bearing LX44 or LX48, daily treatment with 1.5 mg/kg GSK-LSD1 showed 69% and 74% TGI, respectively [3].

T22822

C14H20N2·2HCl

289.2

GSK-LSD1 (hydrochloride)

DMSO:25mg/ml
Ethanol:≤0.1mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years