EP652 is a METTL3 inhibitor and antitumor agent with IC 50 values of 2 nM, <10 nM, and 37 nM in SPA, intracellular, and ATPlite assays, respectively. EP652 exhibits high selectivity against 40 other methyltransferases and FTO , and possesses favorable pharmacokinetic parameters. EP652 reduces intracellular N 6 -methyladenosine (m 6 A) levels in mRNA . EP652 inhibits tumor growth and progression of both hematologic malignancies and solid tumors. EP652 can be used for the research of acute myeloid leukemia, ovarian cancer , non-small cell lung cancer , and hypopharyngeal squamous cell carcinoma.
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