shmt

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

SHMT-IN-4 (Compound 9ay) is a herbicide that specifically targets and inhibits the enzyme serine hydroxymethyltransferase (SHMT1), with an IC50 value of 193.8 g a.i./ha. It functions by binding to SHMT1, thereby disrupting amino acid synthesis and metabolism within plants, which inhibits their growth. Additionally, SHMT-IN-4 exhibits minimal toxicity towards corn and bees.

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.

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.

SHMT2-IN-1 is a potent inhibitor of serine hydroxymethyltransferase 2 (SHMT2) with an IC50 of 1.21 μM and a KD of 10.6 μM. It binds to the folate binding site of SHMT2 and also inhibits SHMT1 with an IC50 of 1.83 μM. MT-44 can suppress the proliferation, migration, and invasion of cancer cells, inducing apoptosis and reactive oxygen species (ROS) production, leading to G2/M phase arrest. SHMT2-IN-1 is applicable in cancer research, including studies on esophageal cancer.

(Rac)-SHIN2, a serine hydroxymethyltransferase (SHMT) inhibitor, enhances NOTCH1-driven in vivo survival of primary T-ALL in mice and is useful for studying T-cell acute lymphoblastic leukemia (T-ALL).

Folinic acid calcium (Leucovorin Calcium) is the active metabolite of folic acid. Leucovorin is used principally as an antidote to folic acid antagonists.

SHIN1 (RZ-2994) is an inhibitor of human serine hydroxymethyltransferse 1(SHMT1) with IC50 of 5 nM and human serine hydroxymethyltransferse 2 (SHMT2) with an IC50 of 13 nM.

AGF347 is a potent multitarget antifolate that acts on serine hydroxymethyltransferase (SHMT)2 located in mitochondria and SHMT1 in the cytoplasm, while inhibiting de novo purine synthesis. This compound induces apoptosis, suppresses the mTOR signaling pathway, reduces glutathione (GSH) levels, and increases reactive oxygen species (ROS) production. AGF347 effectively inhibits the proliferation of both Cisplatin-sensitive and resistant epithelial ovarian cancer (EOC) cells and demonstrates antitumor activity in SKOV3 EOC xenograft mouse models. It is a valuable agent for ovarian cancer research.

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].