gsk 3685032

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

(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.

(S)-GSK-3685032 is an isomer of GSK-3685032 and serves as a control compound in experiments. GSK-3685032 is a selective inhibitor of DNMT1, characterized by its non-time-dependent, non-covalent, and reversible nature, with an IC50 of 0.036 μM. It induces loss of DNA methylation, transcription activation, and inhibition of cancer cell growth.