DDP-38003 dihydrochloride

Description: DDP-38003 dihydrochloride, a tranylcypromine (TCPA) derivative, is a novel, potent and orally bioavailable inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1). DDP-38003 inhibits KDM1A with an IC50 of 84 nM. DDP-38003 is more active in reducing the colony forming ability and in inducing thedifferentiation of THP-1 cells compared to the 1R, 2S analogue. It exhibited in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia model with evidence of KDM1A inhibition. The biological profile of DDP-38003 supports its further investigation as a cancer therapeutic.

References: J Med Chem. 2016 Feb 25; 59(4):1501-17.