Description: (R)-GSK-3685032 is the R-enantiomer of GSK-3685032, a first-in-class, non-time-dependent, non-covalent, reversible, selective DNMT1 inhibitor with an IC50 of 0.036 µM, which induces robust loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth. Target: Others. Smiles:...

A DNMT1 inhibitor (IC50 = 0.23 µM), selective for DNMT1 over DNMT3A/3L and DNMT3B/3L and a panel of 34 methyltransferases and 369 kinases (IC50s = >10 µM for all), inhibits the proliferation of 51 hematological cancer cell lines (median IC50 = 0.64 µM), decreases overall DNA methylation and gene expression in...