cis-4-Br-2,5-F2-PCPA (S1024) 抑制 LSD1 和 LSD2，Ki 值分别为 94 nM 和 8.4 μM。癌症干细胞中LSD1异常表达，cis-4-Br-2,5-F2-PCPA 能够通过增加 CCRF-CEM 细胞中二甲基化组蛋白 H3 的 K4 (H3K4) 水平，抑制LSD1活性和癌细胞增殖。

cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells [1].

cis-4-Br-2,5-F2-PCPA (compound 7c) inhibits proliferation of the T-cell acute lymphoblastic leukemia (T-ALL) with IC 50 s of 12 μM (CCRF-CEM) and 16 μM (Jurkat) respectively, with no inhibitory effect on human normal fibroblast cell line WI-38 [1]. cis-4-Br-2,5-F2-PCPA (20 μM; 24 h) significantly increases the level of dimethylated H3K4 (H3K4me2), and exerts chemical inhibition on LSD1 and LSD2 [1]. Western Blot Analysis [1] Cell Line: T-cell acute lymphoblastic leukemia (T-ALL) Concentration: 20 μM Incubation Time: 24 hours Result: Increased the level of dimethylated H3K4 (H3K4me2) 2.9-fold compared with control.

C9H8BrF2N

248.07

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years