General description
A cell-permeable, 2-PCPA derivative that elicits mechanism based inhibition of 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 inhibition (KI = 110 µM, kinact/KI = 60 (M-1S-1)), with higher potency and selectivity compared with 2-PCPA, 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.
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.
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
Molecular Weight: 311.75. Empirical Formula: C16H16ClF2NO. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51171521
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 489477-5MG