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. Author manuscript; available in PMC: 2019 Jan 4.
Published in final edited form as: Org Lett. 2015 Apr 27;17(10):2326–2329. doi: 10.1021/acs.orglett.5b00737

Figure 2.

Figure 2.

(a) Schematic for cell-based assay of antihypoxic effects of 2-KG esters. A cell line stably expressing a HIF-luciferase gene fusion is treated with cell permeable 2-KG esters. Literature precedent suggests delivery of 2-KG can increase the activity of 2-KG dependent dioxygenases, including PHD2, the prolyl hydroxylase responsible for HIF degradation. (b) Quantitative analysis of cellular antihypoxic activity of 2-KG esters (1 mM). All values are normalized to the average HIF-Luciferase activity of untreated control cells (set at 100%). Compounds 1 and 3 reduce HIF-Luc luciferase activity, consistent with 2-KG release and dioxygenase activation. Values represent the average of three biological replicates, ± standard deviation.