Figure 5.
Butyrate specifically and noncompetitively inhibits PHD2181-402. (a) Representative percentage of PHD2181-402 activity normalized to control based on succinate production following a 10-minute reaction of 1 μM PHD2181-402, 10 μM 2-OG, 10 μM Fe (II), 10 μM HIF-1α547-581 peptide (CODD), and 100 μM ascorbic acid in the presence of 195.3 μM to 100 mM SCFAs (acetate, propionate, butyrate, valerate, and hexanoate) and 78 μM to 40 mM DMOG (n = 4, error bars: SEM, [Inhibitor] vs. normalized response – variable slope least squares fit). (b) True IC50 values for SCFAs and DMOG calculated from measured IC50 values accounting for percentage of substrate conversions between replicate experiments (n = 5–12, error: SEM)