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

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

目录号: HY-151190
产品使用指南

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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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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM IC50
12 μM
Compound: 7c
Anti-proliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay
Anti-proliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay
[PMID: 36105323]
Jurkat IC50
16 μM
Compound: 7c
Anti-proliferative activity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay
Anti-proliferative activity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay
[PMID: 36105323]
WI-38 IC50
> 50 μM
Compound: 7c
Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay
Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay
[PMID: 36105323]
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.

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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