2. Epigenetics
  3. Histone Demethylase
  4. LSD1-IN-46

LSD1-IN-46 是一种强效且具有口服活性的赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂，IC50 值为 0.082 μM。LSD1-IN-46 可阻断 β-catenin 介导的转录程序，从而抑制胃癌细胞的干性。LSD1-IN-46 具有显著的抗肿瘤活性，可用于胃癌的研究。

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LSD1-IN-46

LSD1-IN-46 Chemical Structure

CAS No. : 2982716-97-0

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LSD1-IN-46 相关抗体

Top Publications Citing Use of Products

查看 Histone Demethylase 亚型特异性产品:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LSD1-IN-46 is a potent and orally active Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.082 μM. LSD1-IN-46 interrupts the β-catenin-mediated transcriptional program, thereby suppressing the stemness of gastric cancer cells. LSD1-IN-46 exhibits strong anti-tumor activity. LSD1-IN-46 can be used for the research of gastric cancer[1].
IC50 & Target[1]

LSD1

0.082 μM (IC50)

体外研究
(In Vitro)

LSD1-IN-46 (Compound X-1) (0.5-2 μM; 5 days) 会增加 MKN-45 细胞中 H3K4me1/2 的水平，而这种效应在 LSD1 敲除细胞中不存在[1]。

LSD1-IN-46 (0.5-2 μM; 5 days) 抑制 MKN-45 细胞自我更新、球形成和集落形成能力，下调 β-catenin、c-Myc 及干细胞标志物 OCT4、NANOG、SOX2 的表达[1]。

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

LSD1-IN-46 相关抗体:

Western Blot Analysis[1]

Cell Line: MKN-45
Concentration: 0.5, 1, 2 μM
Incubation Time: 5 days
Result: Decreased OCT4, NANOG, and SOX2 levles.
Downregulated the expression of β-catenin, c-Myc.
体内研究
(In Vivo)

LSD1-IN-46 (Compound X-1) (10-20 mg/kg； 口服灌胃； 每日一次； 持续 11 天) 减少 BALB/c 裸鼠皮下注射 MFC 胃癌细胞的肿瘤大小和重量[1]。

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

Animal Model: BALB/c nude mice with injection of MFC gastric cancer cells (male, 6-8 weeks old)[1]
Dosage: 10, 20 mg/kg
Administration: Oral gavage; Once daily; 11 days
Result: Reduced tumor size and weight.
Did not affect mouse body weight or causing obvious hepatorenal toxicity.
Downregulated the expression of β-catenin, c-Myc, SOX2, NANOG in tumor tissues.
分子量

351.49

Formula

C22H29N3O
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

LSD1-IN-46 相关分类

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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.

Keywords:

LSD1-IN-462982716-97-0Histone DemethylaseMFC MKN-45 H3K4me β-catenin c-Myc OCT4 NANOG SOX2Inhibitorinhibitorinhibit

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