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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
35 μM
Compound: 5
Cytotoxicity against human A549 cells after 48 hrs by resazurin reduction assay
Cytotoxicity against human A549 cells after 48 hrs by resazurin reduction assay
[PMID: 20413315]
DLD-1 IC50
74 μM
Compound: 5
Cytotoxicity against human DLD1 cells after 48 hrs by resazurin reduction assay
Cytotoxicity against human DLD1 cells after 48 hrs by resazurin reduction assay
[PMID: 20413315]
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
性状

固体

颜色

Light yellow to green yellow

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (87.63 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5052 mL 17.5260 mL 35.0521 mL
5 mM 0.7010 mL 3.5052 mL 7.0104 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5052 mL 17.5260 mL 35.0521 mL 87.6301 mL
5 mM 0.7010 mL 3.5052 mL 7.0104 mL 17.5260 mL
10 mM 0.3505 mL 1.7526 mL 3.5052 mL 8.7630 mL
15 mM 0.2337 mL 1.1684 mL 2.3368 mL 5.8420 mL
20 mM 0.1753 mL 0.8763 mL 1.7526 mL 4.3815 mL
25 mM 0.1402 mL 0.7010 mL 1.4021 mL 3.5052 mL
30 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9210 mL
40 mM 0.0876 mL 0.4382 mL 0.8763 mL 2.1908 mL
50 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7526 mL
60 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
80 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0954 mL
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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Arborinine
目录号:
HY-128912
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