(r)gsk3685032

(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.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.