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 DNA and inhibit DNMT1, DNMT3A, and DNMT3B irreversibly, and as a consequence are toxic [...]
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Nov. 26, 2021
GSK3685032: A First-In-Class DNMT1 Inhibitor
GSK3685032
selective rev. DNA methyltransferase inhibitor preclinical eff. at 30 mpk SC BID (xenograft) from 1.8M cmpd enzymatic HTS + opt. Nature Cancer GlaxoSmithKline