产品说明
一般描述
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.
包装
5 mg in Glass bottle
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Mimasu, S., et al. 2010. Biochemistry49, 6494.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C16H16ClF2NO |
分子量 | 311.75 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze |
颜色 | white |
溶解性 | DMSO: 100 mg/mL water: 25 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich