GOT1 inhibitor-1GOT1 inhibitor-1
MedChemExpress (MCE)
HY-122723
732973-87-4
99.45%
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 plays an important role in energy metabolism and Reactive Oxygen Species (ROS) balance. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1 (glutamate-oxaloacetate transaminase 1 (GOT1)), for the maintenance of redox homeostasis and sustained proliferation. Small molecule inhibitors targeting this metabolic pathway may provide a novel way for cancer research. In the MDH coupled GOT1 enzymatic assay, GOT1 inhibitor-1 shows an inhibitory effect on GOT1 activity with an IC50 value of 8.2 uM[1].
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[1]. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1
28(16):2675-2678 [Content Brief]
[2]. Sun W, et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun Signal. 2019
17(1):111. [Content Brief]