HDAC1

673nM(IC₅₀,30min(time-dependent))

PDE5

114nMnM(IC₅₀)

CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer's disease[1].

CM-675 (29a) shows a significant time-dependent effect on class I HDAC inhibition, particularly towards HDAC2. For HDAC1, its inhibitory potency also increased significantly (~1 log unit) with the pre-incubation time: 673 nM (30 min), 180 nM (4 hours) and 69 nM (6 hours) [1].

[1]. Rabal O, et al. Discovery of in Vivo Chemical Probes for Treating Alzheimer's Disease: Dual Phosphodiesterase 5 (PDE5) and Class I Histone Deacetylase Selective Inhibitors. ACS Chem Neurosci. 2019 Mar 20;10(3):1765-1782.