2. Epigenetics
  3. Histone Demethylase
  4. cis-4-Br-2,5-F2-PCPA

cis-4-Br-2,5-F2-PCPA  (Synonyms: S1024)

目录号: HY-151190
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摩尔计算器

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。

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

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

CAS No. : 2821068-03-3

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cis-4-Br-2,5-F2-PCPA 相关抗体

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

  • 生物活性

  • 纯度 & 产品资料

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生物活性

cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. 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].

IC50 & Target

KDM1/LSD1

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

cis-4-Br-2,5-F2-PCPA 相关抗体:

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
CAS 号
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.
纯度 & 产品资料
参考文献

cis-4-Br-2,5-F2-PCPA 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

cis-4-Br-2,5-F2-PCPA2821068-03-3S1024S 1024S-1024Histone Demethylasedemethylates mono- and dimethylated lysineH3K4H3K9T-cell acute lymphoblastic leukemiaT-ALL2-phenylcyclopropylaminePCPAInhibitorinhibitorinhibit

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