trans CM-414

A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM); does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM); diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice.

References 1. Cuadrado-Tejedor M, et al. Neuropsychopharmacology. 2017 Jan;42(2):524-539. View Related Products by Target HDAC