got1

GOT1 inhibitor-1 (GOT1 inhibitor 2c) is a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM.

iGOT1-01 is an effective inhibitor of glutamate oxaloacetate transaminase 1(GOT1) . iGOT1-01 has IC50s of 84.6 μM and 11.3 μM in GOT1/MDH1 assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 can be used in anti-cancer studies.

Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) reduces tumor growth in an SW1990 mouse xenograft model. |1. Zhang, P., Li, X.-M., Wang, J.-N., et al. New butenolide derivatives from the marine-derived fungus Paecilomyces variotii with DPPH radical scavenging activity. Phytochem. Lett. 11, 85-88 (2015).|2. Sun, W., Luan, S., Qi, C., et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun. Signal. 17(1), 111 (2019).

Aspulvinone H is a natural inhibitor of glutamic oxaloacetate transaminase 1 (GOT1), suppressing glutamine metabolism, making PDAC cells sensitive to oxidative stress and inhibiting cell proliferation, exhibiting potent in vivo antitumor activity in an SW1990-cell-induced xenograft model.