ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).

JMJD2:920 nM

ML324 exhibits good Caco-2 cell permeability, and possesses excellent microsomal stability in the presence of both mouse and rat liver microsomes. ML324 demonstrates potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection by inhibiting viral IE gene expression. [1]

In a mouse ganglia explant model of latently infected mice, ML324 suppresses the formation of HSV plaques, and blocks HSV-1 reactivation. [1]

The fluorescence resonance energy transfer (FRET)-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the Km values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are then recorded[1].