Description |
A cell-permeable, 2-PCPA derivative that elicits mechanism based inhibition of LSD1 (IC 50 = 0.99 µM, K I = 0.61 µM, and k inact /K I = 4560 (M -1 S -1 )), and displays much lower inhibition activity toward MAO-B (K I = 17 µM, k inact /K I = 18 (M -1 S -1 )) and MAO-A inhibition (K I = 110 µM, k inact /K I = 60 (M -1 S -1 )), with higher potency and selectivity compared with 2-PCPA, IC 50 = 184 µM, K I = 100 µM, k inact /K I = 58 (M -1 S -1 )) for LSD1, and K I = 26 µM, k inact /K I = 271 (M -1 S -1 )) for MAO-B, and K I = 5 µM, k inact /K I = 1050 (M -1 S -1 )) for MAO-A)
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