489477

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.

• Synonym(s): LSD1 Inhibitor II, S2101, S2101, LSD Inhibitor II, BHC110 Inhibitor II, Histone Lysine Demethylase Inhibitor IV, KDM1 Inhibitor II, MOA Inhibitor II
• Empirical Formula (Hill Notation): C₁₆H₁₆ClF₂NO
• Molecular Weight: 311.75
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: white
• solubility: DMSO: 100 mg/mL; water: 25 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

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.

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable