MilliporeSigma™ Calbiochem™ LSD1 Inhibitor II, S2101

Description

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

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

• Color: White
• Description: 95% by HPLC
• Molecular Formula: C₁₆H₁₆ClF₂NO
• Formula Weight: 311.75g/mol
• Solubility: DMSO or H₂O
• Form: Solid
• Quantity: 5 mg