Chemical structure of molecule GSK3685032

selective rev. DNA methyltransferase inhibitor

preclinical eff. at 30 mpk SC BID (xenograft)

from 1.8M cmpd enzymatic HTS + opt.

Nature Cancer


The GSK DNMT1 inhibitor GSK3685032 is a first-in-class, non-nucleoside, reversible and selective inhibitor of the epigenetic target DNA-methyltransferase 1 (DNMT1). Commonly prescribed hypomethylating agents (HMAs) such as decitabine are incorporated into…

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