| Bioactivity | iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC50s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity[1][2]. | ||||||||||||
| Target | IC50: 85 μM (MDH coupled GOT1 enzymatic assay) and 11.3 μM (GOT1/GLOX/HRP assay) | ||||||||||||
| Invitro | iGOT1-01 has an IC50 of 84.6 μM in the GOT1/MDH1 assay. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM[2]. iGOT1-01 (3.125-200 μM; for 3 h) reveals little to no toxicity using two readouts of cell viability in PaTu8902 pancreatic and DLD1 colon cancer cells[2]. | ||||||||||||
| In Vivo | iGOT1-01 (compound 1a; 20 mg/kg; oral) has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour•ng/mL)[1]. Animal Model: | ||||||||||||
| Name | iGOT1-01 | ||||||||||||
| CAS | 882256-55-5 | ||||||||||||
| Formula | C19H20N4O | ||||||||||||
| Molar Mass | 320.39 | ||||||||||||
| 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. [2]. Melissa C Holt, et al. Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors. Biochemistry. 2018 Nov 27;57(47):6604-6614. |