shmt 1

SHMT-IN-1 is a potent plasmodial serine hydroxymethyltransferase (SHMT) inhibitor with antitumor activity.

SHMT-IN-2 (compound 2) is a specific human SHMT1/2 small molecule inhibitor that acts on SHMT1 (IC50: 13 nM) and SHMT2 (IC50: 66 nM). SHMT-IN-2 inhibits the growth of many human cancer cells and is sensitive to B-cell lymphoma.

SHMT-IN-3 (Hit 1) is an inhibitor of SHMT1 and SHMT2, exhibiting an IC50 value of 0.53 µM for human SHMT1. It acts as a non-competitive inhibitor with respect to serine.

D-homoserine lactone is an enantiomer of L-homoserine lactone and an inhibitor of serine hydroxymethyltransferase (SHMT; Ki= 11 mM for the rabbit enzyme).1 1.Wang, E.A., Kallen, R., and Walsh, C.Mechanism-based inactivation of serine transhydroxymethylases by D-fluoroalanine and related amino acidsJ. Biol. Chem.256(13)6917-6926(1981)

(+)SHIN2, an isomer of (-)SHIN2, is an inhibitor of serine hydroxymethyltransferase (SHMT) with antileukemic effects and shows synergistic activity with Methotrexate in in vivo xenotransplantation models [1].