Bioactivity | 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 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC)[1]. | |||||||||
Invitro | 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]. | |||||||||
Name | GOT1 inhibitor-1 | |||||||||
CAS | 732973-87-4 | |||||||||
Formula | C19H19ClN4O | |||||||||
Molar Mass | 354.83 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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 |