SHMT Inhibitor

SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC₅₀s of 5 and 13 nM, respectively, in an in vitro assay.

(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with ¹³C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519). (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

SHMT-IN-2 is a stereo specific inhibitor of human SHMT1/2 with IC₅₀ values of 13 nM and 66 nM for SHMT1 and SHMT2, respectively. SHMT-IN-2 can block the growth of many human cancer cells, and has sensitivity for B-cell lymphomas.

(Rac)-SHIN2 is a pyrazolopyran derivative and a serine hydroxymethyltransferase (SHMT) inhibitor. (Rac)-SHIN2 has antibacterial activity and low cytotoxicity against Hep2 cells. (Rac)-SHIN2 exerts potent antibacterial activity against both vancomycin-susceptible and vanA-type vancomycin-resistant Enterococcus.

(+)-SHIN1 ((+)-RZ-2994) is an active (+) enantiomer of SHIN1.

AGF347 is a potent and multi-targeted antifolate that targets serine hydroxymethyltransferase (SHMT)2 in the mitochondria and SHMT1 in the cytosol, and inhibits de novo purine biosynthesis. AGF347 induces apoptosis, inhibits mTOR signaling, decreases GSH pools, and increases ROS. AGF347 inhibits proliferation of Cisplatin (HY-17394) sensitive and resistant epithelial ovarian cancer (EOC) cells. AGF347 exhibits antitumor efficacy in SKOV3 EOC xenograft mouse models. AGF347 can be used for ovarian cancer research.

Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP⁺ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric cancer.

SHMT-IN-1 is a Plasmodium falciparum Serine Hydroxymethyltransferase (PfSHMT) inhibitor with an IC₅₀ of 350 nM. SHMT-IN-1 can be used for the research of malaria.

(-)SHIN2 is the isomer of (+)SHIN2 (HY-134978A). (+)SHIN2 is an inhibitor of serine hydroxymethyltransferase (SHMT) with antileukemic effect. (+)SHIN2 synergisty with and Methotrexate (HY-14519) in vivo xenotransplantation models. (-)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 (SHMT2) inhibitor with an IC₅₀ of 1.21 μM and a K_D of 10.6 μM. SHMT2-IN-1 binds to the folate binding site of SHMT2. SHMT2-IN-1 also inhibits SHMT1 with an IC₅₀ of 1.83 μM. SHMT2-IN-1 can inhibit cancer cells proliferation, migration and invasion. SHMT2-IN-1 can induce cells apoptosis and ROS production and cause G2/M phase arrest. SHMT2-IN-1 can be used for the research of cancer, such as esophageal cancer.

SHMT-IN-3 (Hit 1) is a SHMT1 and SHMT2 inhibitor with an IC50 of 0.53 µM for human SHMT1. SHMT-IN-3 exhibits noncompetitive inhibition against serine.

SHMT-IN-4 (Compound 9ay) is a herbicide that targets and inhibits serine hydroxymethyltransferase (SHMT1) with an IC₅₀ value of 193.8 g a.i./ha (active ingredient content per hectare). SHMT-IN-4 interferes with amino acid synthesis and metabolism in plants by binding to SHMT1, thereby inhibiting plant growth. Additionally, SHMT-IN-4 shows no significant toxicity to maize and honeybees.