1. Epigenetics
  2. Histone Demethylase
  3. LSD1/2-IN-3

LSD1/2-IN-3 是赖氨酸特异性去甲基化酶 1 (LSD1) 的选择性抑制剂,Ki 为 11 nM,而对 LSD2 的 Ki 值为 7 μM。LSD1 在癌干细胞中异常表达,LSD1/2-IN-3 能够抑制 LSD1 活性和癌细胞增殖。

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LSD1/2-IN-3 Chemical Structure

LSD1/2-IN-3 Chemical Structure

CAS No. : 2821068-07-7

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查看 Histone Demethylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation[1].

IC50 & Target

KDM1/LSD1

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM IC50
25 μM
Compound: 8c
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
27 μM
Compound: 8c
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: 8c
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)

LSD1/2-IN-3 (compound 8c) inhibits proliferation of the T-cell acute lymphoblastic leukemia (T-ALL) with IC50s of 25 μM (CCRF-CEM) and 27 μM (Jurkat), respectively, without inhibiting the human normal fibroblast cell line WI-38[1].

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

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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产品名称:
LSD1/2-IN-3
目录号:
HY-151192
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