LSD1 Inhibitor II, S2101 – Calbiochem

Descrição detalhada : A cell-permeable, 2-PCPA derivative that elicits mechanism-based inhibition against LSD1 (IC50 = 0.99 µM, KI = 0.61 µM, and kinact/KI = 4560 M-1S-1), and displays much lower inhibition activity toward MAO-B (KI = 17 µM, kinact/KI = 18 M-1S-1) and MAO-A (KI = 110 µM, kinact/KI = 60 M-1S-1), with higher potency and selectivity compared with those of 2-PCPA (Cat. No. 616431) (IC50 = 184 µM, KI = 100 µM, kinact/KI = 58 M-1S-1 for LSD1, and K I = 26 µM, kinact/KI = 271 M-1S-1 for MAO-B, and K I = 5 µM, kinact/KI = 1050 M-1S-1 for MAO-A). The inhibition of LSD1 is further confirmed in a cell-based assay, the treatment of HEK293T human cells with S2101 results in a dose-dependent increase in the level of H3K4me2, and about 50-fold stronger inhibition compared with that of 2-PCPA., A cell-permeable, 2-PCPA derivative that elicits mechanism based inhibition of LSD1 (IC50 = 0.99 µM, KI = 0.61 µM, and kinact/KI = 4560 (M-1S-1)), and displays much lower inhibition activity toward MAO-B (KI = 17 µM, kinact/KI = 18 (M-1S-1)) and MAO-A inhibition (KI = 110 µM, kinact/KI = 60 (M-1S-1)), with higher potency and selectivity compared with 2-PCPA, IC50 = 184 µM, KI = 100 µM, kinact/KI = 58 (M-1S-1)) for LSD1, and K I = 26 µM, kinact/KI = 271 (M-1S-1)) for MAO-B, and K I = 5 µM, kinact/KI = 1050 (M-1S-1)) for MAO-A). The inhibition of LSD1 is further confirmed in a cell based assay, the treatment of HEK293T human cells with S2101 results in a dose-dependent increase in the level of H3K4me2, and about 50-fold stronger inhibition compared with that of 2-PCPA.
Sinónimos : LSD1 Inhibitor II, S2101 - Calbiochem; S2101, LSD Inhibitor II, BHC110 Inhibitor II, Histone Lysine Demethylase Inhibitor IV, KDM1 Inhibitor II, MOA Inhibitor II
Fórmula molecula r: C16H16ClF2NO
Armazenamento : 2-8C; 2-8C
Embalagem : 1X5MG