Inhibition of serine/glycine synthesis by SHMT inhibitors can be an effective strategy to treat serine/glycine synthesis-dependent cancers. Therefore, SHMT inhibitor can be a potential cancer drug target. SHMT inhibitor Hit 1 may inhibit SHMT with anIC50 of 0.53??M.
SHMT inhibitor Hit 1 is a potent and specific inhibitor of serine hydroxymethyltransferase (SHMT). SHMT inhibitor Hit 1 potently inhibits SHMT1 and SHMT2 in rat liver homogenate.