中文名称: Inauhzin
英文名称: Inauhzin
CAS No: 309271-94-1
分子式: C25H19N5Os2
分子量: 469.58
I10168 Inauhzin ≥98%(HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(20mg/mL 加热 超声)
产品描述:

基本信息

产品编号:I10168

产品名称:Inauhzin

CAS:

309271-94-1

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C25H19N5Os2

溶于液体

-80℃

两年

分子量

469.58

-20℃

一个月

化学名: 

2-((5H-[1,2,4]triazino[5,6-b]indol-3-yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one

 

Solubility (25°C)

 

体外

DMSO

94mg/mL (200.17mM)

Ethanol

Insoluble

Water

Insoluble

体内

现配现用

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.1296mL

10.6478mL

21.2956mL

5mM

0.4259mL

2.1296mL

4.2591mL

10mM

0.2130mL

1.0648mL

2.1296mL

50mM

0.0426mL

0.2130mL

0.4259mL

 

生物活性

产品描述

一种SirT1/IMPDH2的双重抑制剂,同时为p53的激活剂。

靶点/IC50

SIRT1 
()

p53 
()

 

体外研究

Inauhzin (10µM) induces p53 levels as effectively as actinomycin D (10nM), and mediates p53-dependent cytotoxicity through its specific functional groups in human lung carcinoma H460 cells. Inauhzin (2µM) induces p53 level and activity as well as p53-dependent apoptosis. Inauhzin also stabilizes p53 and inhibits its ubiquitylation. Inauhzin induces acetylation of p53 in H460 cells, but not tubulin, which is affected by knockdown of SIRT1. Inauhzin (0-2 µM) significantly enhances the expression level and activity of p53 in HCT116p53+/+ cells and enhances the expression level and activity of p53 in H460 cells in a dose-dependent manner. Inauhzin and Nutlin-3 demonstrate synergistic cytotoxicity in the Nutlin-3 low-sensitive cells.

Inauhzin and Nutlin-3 synergistically induce p53-dependent apoptosis. Inauhzin targets both SirT1 and IMP dehydrogenase 2 (IMPDH2), and acts as a potent p53 activator.

 

体内研究

Inauhzin (30mg/kg, i.p.) effectively induces apoptosis and suppresses tumour growth of H460 xenograft harbouring p53.

Inauhzin (30mg/kg, i.p.) reduces the HCT116 tumor volume by appr 70%. Inauhzin (15mg/kg) in combination with 150mg/kg of Nutlin-3 demonstrates a significant synergy on p53 induction, apoptosis and tumor suppression of HCT116p53+/+ xenografts.

 

推荐实验方法(仅供参考)

细胞实验:

Cell Assay

The cell counting kit is used to assess cell growth. Cell suspensions are seeded at 5000 cells per well in 96-well culture plates and incubated overnight at 37°C. Compounds are added into the plates and incubated at 37°C for 72 h. Cell growth inhibition is determined by adding WST-8 at a final concentration of 10% to each well, and the absorbance of the samples is measured at 450nm using a Microplate Reader.

 

动物实验:

 

Animal Administration

Five-weeks-old female SCID mice are housed in a BSL2 environment. Mice are subcutaneously inoculated with 5×106 H460 or 3×106 HCT116 cells. Tumour growth is monitored every other day with electronic digital calipers in two dimensions.Tumour volume is calculated with the formula: tumour volume (mm3) = (length × width2)/2. When the mean tumour volume reaches approximately 100 mm3 after 7-9 days, animals are dosed by i.p. injection with vehicle (5% DMSO) or Inauhzin. Inhibition of tumour growth is calculated on the last day of treatment. To detect p53 activation in vivo, tumours are harvested and disrupted in RIPA buffer containing a protease inhibitor mixture. Tumour lysates are analysed by IB. Cell proliferation in tumours is assessed by BrdU labeling followed by Immunostaining. 200mg/kg body weight of BrdU is administrated to mice via i.p. injection 2 h before mice are sacrificed. Apoptosis is examined by TUNEL staining, using the Fluorescein In situ cell death detection kit

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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稀释公式

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连续稀释计算器方程

  • 连续稀释

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  • 稀释倍数:
  • 计算结果

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    C8=C7/X C8: LOG(C8):