DNA methylation regulates gene expression in normal and malignant cells. RG108 is a non-nucleoside DNA methyltransferase inhibitor (IC50 = 115 nM in vitro). It significantly reduces the methylation of genomic DNA in cells at 10 µM without detectable toxicity, distinguishing it from nucleoside-based inhibitors like...

1-NM-PP1 is a cell permeable inhibitor of kinases that have been mutated, by a single base substitution, to become 'analog sensitive' (as), as compared to the wild-type kinase. 1-NM-PP1 was first developed to optimally inhibit v-Src-as1, with an I338G substitution, preferentially over v-Src (IC50 = 4.2 nM versus 28...

Bisindolylmaleimide V (BIM V) is a weak inhibitor of protein kinase C (PKC) demonstrating an IC50 value >100 µM. While effectively inactive as a PKC inhibitor, BIM V blocks the activation of mitogen-stimulated protein kinase p70s6k/p85s6k (S6K) in vivo with an IC50 value of 8 µM.Formal Name:...