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. 2011 Oct 17;6(10):e26338. doi: 10.1371/journal.pone.0026338

Figure 2. Activation status of PKC changes the inhibition kinetics of BIS I but not BIS IV.

Figure 2

(A) Oxo-M responses with (closed circles) or without (open circles) BIS I in the quiescent condition. The boxes indicate the presence of 200 nM BIS I (grey) and 3 µM oxo-M (black). (B) Oxo-M responses with (closed circles) or without (open circles) BIS I in the preactivated condition. Cells were treated sequentially with 100 nM phorbol 12,13-dibutyrate (PDBu) (open box), 200 nM BIS I (grey box), and 3 µM oxo-M (black box). (C) Relative peak oxo-M responses from experiments similar to (A) and (B) with various incubation times with BIS I. Peak oxo-M responses under various BIS I incubation times are normalized to the peak response without BIS I treatment (t = 0). For instance, (A) represents two data points for the PDBu(–) condition, t = 0 min (no inhibitor, n = 19) and t = 5 min (BIS I, n = 14). (B) represents two data points for the PDBu(+) condition, t = 0 (no inhibitor, n = 15) and t = 5 min (BIS I, n = 15). Preactivation with PDBu (closed circles) facilitates PKC inhibition by BIS I compared to no PDBu (open circles). (D) Oxo-M responses with (closed circles) or without (open circles) 1 µM BIS IV in the quiescent condition. The control is the same as in (A). (E) Oxo-M responses with (closed circles) or without (open circles) 1 µM BIS IV in the preactivated condition. The control is the same as in (B). (F) Time course of relative peak oxo-M responses showing inhibition kinetics of BIS IV for preactivated PKC (closed circles) and the control (open circles) from experiments similar to (D) and (E) with various incubation times with BIS IV. Relative peak oxo-M responses with various incubation time with BIS IV are calculated using response at t = 0 as a reference. Panel (D) represents two data points for the PDBu(–) condition, t = 0 (no inhibitor, n = 19) and t = 5 min (BIS IV, n = 15). Panel (E) represents two data points for the PDBu(+) condition, t = 0 (no inhibitor, n = 15), and t = 5 min (BIS IV, n = 9).