3-Bromopyruvate completely inhibits SHMT1, alkylating the active site Cys204.
SHMT2, which lacks Cys 204, is only partially inhibited by 3-bromopyruvate.
3-Bromopyruvate binds to SHMT1 active site forming a non-covalent complex.
Introducing a Cys residue in SHMT2 active site yields a complete inhibition.
3-Bromopyruvate is a lead compound for the design of selective SHMT1 inhibitors.