cis-4-Br-2,5-F2-PCPA

立即咨询

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

S1024

产品介绍

cis-4-Br-2,5-F2-PCPA (S1024) 是赖氨酸特异性去甲基化酶 1 (LSD1) 的选择性抑制剂，K_i为 94 nM，而对LSD2的 K_i值为 8.4 μM。LSD1在癌干细胞中异常表达，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。

生物活性

cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor oflysine-specific demethylase 1(LSD1), with aK_ivalue of 94 nM instead of 8.4 μM forLSD2. There is aberrant expression ofLSD1incancer stem cells, cis-4-Br-2,5-F2-PCPA inhibitsLSD1cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells^[1].

IC₅₀& Target

Ki: 94 nM (LSD1); 8.4 μM (LSD2)^[1]

体外研究
(In Vitro)

cis-4-Br-2,5-F2-PCPA (compound 7c) inhibits proliferation of the T-cell acute lymphoblastic leukemia (T-ALL) with IC₅₀s of 12 μM (CCRF-CEM) and 16 μM (Jurkat), respectively, without inhibiting the 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.

分子量

248.07

Formula

C₉H₈BrF₂N

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.