Key Specifications Table
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|489477-5MG||Glass bottle||5 mg||
|Overview||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.
|Synonyms||S2101, BHC110 Inhibitor II, Histone Lysine Demethylase Inhibitor IV, KDM1 Inhibitor II, MOA Inhibitor II, LSD Inhibitor II|
|References||Mimasu, S., et al. 2010. Biochemistry 49, 6494.|
|Structure formula Image|
|Application||LSD1 Inhibitor II, S2101, is a cell-permeable, 2-PCPA derived mechanism-based inhibitor of LSD1 (IC50 = 0.99 µM, KI = 0.61 µM, and kinact/KI = 4560 M-1S-1).|
|Purity||≥95% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Mimasu, S., et al. 2010. Biochemistry 49, 6494.|