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cis-4-Br-2,5-F2-PCPA
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。
cis-4-Br-2,5-F2-PCPA图片
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,Ki为 94 nM,而对LSD2的 Ki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 aKivalue 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.