1. Epigenetics
  2. Histone Demethylase
  3. Arborinine

Arborinine 是一种有效的口服活性 LSD1 抑制剂。Arborinine 增加 H3K4me1/2、H3K9me1/2、E-cad 蛋白的表达并降低 UBE2O 蛋白水平的表达。Arborinine 诱导细胞周期停滞在 S 期。Arborinine 具有抗肿瘤活性。

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Arborinine Chemical Structure

Arborinine Chemical Structure

CAS No. : 5489-57-6

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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

Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity [1][2].

IC50 & Target[2]

LSD1

 

体外研究
(In Vitro)

Arborinine (0, 5, 15, 30 µM; 48 h) 增加 H3K4me1/2、H3K9me1/2、E-cad 蛋白的表达[1]
Arborinine (20 µM) 降低 786O 细胞中 UBE2O 蛋白水平的表达[1]
Arborinine (20 µM) 诱导细胞周期停滞在 S 期并抑制细胞凋亡[1]

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

Cell Proliferation Assay[1]

Cell Line: 786O, A498, 769P, Caki1, OSRC2 cells
Concentration: 0-100 µM
Incubation Time: 48, 72 h
Result: Showed antiproliferative activity with IC50s of 30.62, 39.09, 15.67, 31.42, 30.35 µM at 48 h, 20.92, 27.01, 14.94, 30.26, 17.37 µM at 72 h for 786O, A498, 769P, Caki1, OSRC2 cells, respectively.

Western Blot Analysis[1]

Cell Line: 786O cells
Concentration: 0, 5, 15, 30 µM
Incubation Time: 48 h
Result: Increased the expression of H3K4me1/2 and H3K9me1/2 protein in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: 786O and A498 cells
Concentration: 20 µM
Incubation Time:
Result: Induced increased population in S phase and decreased population in G1 phase, significantly inhibited both early and late apoptosis of ccRCC cells
体内研究
(In Vivo)

Arborinine (40、80 mg/kg;灌胃; 21 天) 在小鼠体内显示出抗肿瘤活性[2]

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

Animal Model: BALB/c nude mice (SGC-7901 cells and SGC-7901/ADR cells)[2]
Dosage: 40, 80 mg/kg
Administration: P.o.; for 21 days
Result: Inhibited the growth of tumors while unchanged the body weights.
分子量

285.29

Formula

C16H15NO4

CAS 号
结构分类
初始来源

Globigerina parva

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

Arborinine 相关分类

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Help & FAQs
  • 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:
Arborinine
目录号:
HY-128912
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