LSD1 Inhibitor II, S2101

A cell-permeable, 2-PCPA derivative that elicits mechanism based inhibition of LSD1 (IC₅₀ = 0.99 µM, K_I = 0.61 µM, and k_inact/K_I = 4560 (M^-1S^-1)), and displays much lower inhibition activity toward MAO-B (K_I = 17 µM, k_inact/K_I = 18 (M^-1S^-1)) and MAO-A inhibition (K_I = 110 µM, k_inact/K_I = 60 (M^-1S^-1)), with higher potency and selectivity compared with 2-PCPA, IC₅₀ = 184 µM, K_I = 100 µM, k_inact/K_I = 58 (M^-1S^-1)) for LSD1, and K _I = 26 µM, k_inact/K_I = 271 (M^-1S^-1)) for MAO-B, and K _I = 5 µM, k_inact/K_I = 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 against LSD1 (IC₅₀ = 0.99 µM, K_I = 0.61 µM, and k_inact/K_I = 4560 M^-1S^-1), and displays much lower inhibition activity toward MAO-B (K_I = 17 µM, k_inact/K_I = 18 M^-1S^-1) and MAO-A (K_I = 110 µM, k_inact/K_I = 60 M^-1S^-1), with higher potency and selectivity compared with those of 2-PCPA (Cat. No. 616431) (IC₅₀ = 184 µM, K_I = 100 µM, k_inact/K_I = 58 M^-1S^-1 for LSD1, and K _I = 26 µM, k_inact/K_I = 271 M^-1S^-1 for MAO-B, and K _I = 5 µM,
k_inact/K_I = 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.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Mimasu, S., et al. 2010. Biochemistry49, 6494.

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