EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.
ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.
RL71 is a sselective inhibitor of SERCA2, specially binding to SERCA2 at a novel site, suppressing the Ca2+-ATPase activity of SERCA2, inducing apoptosis and downregulating Akt.
FL77-24, an analog of FL118 and an apoptosis inducer, exhibits antitumor activity with IC50 values of 99.4 nM in HCT116 cells, 118 nM in HepG2 cells, less than 6.4 nM in both MCF-7 and HeLa cells, and 28.5 nM in A549 cells. It primarily induces cell cycle arrest in the S and G2 M phases [1].