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MilliporeSigma™ Calbiochem™ LSD1 Inhibitor II, S2101

The LSD1 Inhibitor II, S2101 controls the biological activity of LSD1. This small molecule/inhibitor is primarily used for Cell Signaling applications.

Manufacturer:  MilliporeSigma™ 4894775MG

Catalog No. 48-947-75MG


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Description

Description

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

Specifications

95% by HPLC
5mg
311.75g/mol
White solid
C16H16ClF2NO
DMSO or H2O
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