| HLI 373Hdm2 ubiquitin ligase (E3) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 502137-98-6 | SDF | Download SDF |
| Chemical Name | 5-((3-(dimethylamino)propyl)amino)-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dione dihydrochloride | ||
| Canonical SMILES | O=C(C1=C(NCCCN(C)C)C2=C(N(C)C1=N3)C=CC=C2)N(C)C3=O.Cl.Cl | ||
| Formula | C18H23N5O2.2HCl | M.Wt | 414.33 |
| Solubility | <37.79mg l="" in="" h2o;=""><3.78mg l="" in="" dmso=""> | Storage | Desiccate at RT |
| Physical Appearance | Cream solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: N/A
HLI 373 is an inhibitor of Hdm2 ubiquitin ligase (E3).
Hdm2 ubiquitin ligase(E3) is a major regulator of p53 by promoting its ubiquitylation and proteasomal degradation. Therefore, blocking Hdm2-mediated activities may be a therapeutic approach for cancers expressing wild-type p53 [1].
In vitro: HLI373 effectively induces apoptosis of several tumor cells that are sensitive to DNA-damaging agents. HLI373-treated cells showed significantly more DNA retained on the filter, indicating that it does not induce single-strand break in U2OS cells. Having no discernable effect on gp78 or AO7, HLI373 seems prefer to inhibit the ubiquitin ligase activity of Hdm2. Treatment of U2OS cells with HLI373 at 10 Amol/L also leaded to a marked decrease in ubiquitylated species immunoprecipitated with anti-Hdm2, whereas the level of immunoprecipitated Hdm2 increased. Inhibition of Hdm2-mediated ubiquitylation in cells can trigger stabilization of both p53 and Hdm2 and preferential killing of tumor cells expressing wild-type p53. HLI373 increased p53 through inhibiting Hdm2-mediated ubiquitylation and not by inducing a DNA damage response in U2OS cells. HLI373 has high potency in stabilizing Hdm2 and p53. HLI373 inhibits the ubiquitin ligase activity of Hdm2 and induces a wild-type p53-dependent apoptosis in several tumor cells that are sensitive to DNA-damaging agents [1,2].
In vivo: So far, no study in vivo has been conducted.
Clinical trial: So far, no clinical study has been conducted.
References:[1]. Kitagaki J, Agama KK, Pommier Y, et al. Targeting Tumor Cells Expressing p53 with a Water-soluble Inhibitor of Hdm2. Molecular Cancer Therapeutics, 2008; 7(8): 2445-1454.[2].Yang Y, Kitagaki J, Wang H, Hou DX, Perantoni AO. Targeting the Ubiquitin-proteasome System for Cancer Therapy. Cancer Science, 2009, 100(1): 24-28.
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最后，再请问磷32的危害性有多大？
频率，是单位时间内完成周期性变化的次数，是描述周期运动频繁程度的量，常用符号f或ν表示，单位为秒分之一，符号为s。为了纪念德国物理学家赫兹的贡献，人们把频率的单位命名为赫兹，简称"赫"，符号为Hz。每个物体都有由它本身性质决定的与振幅无关的频率，叫做固有频率。频率概念不仅在力学、声学中应用，在电磁学、光学与无线电技术中也常使用。
因为声的多普勒效应，用专用仪器在空气里测频率似乎变得不可靠。 最简单直接的方法，用频率特性仪，接换能器正负极测量读数 或者拿一片超声波振子接受对方发射的超声波进行放大后，输入到整形电路，再输入到计数器，就可以测量频率了
求助原因：论文答辩
你参与的主要专业版面（必填）：预防医学与医学统计讨论版
试验或调查设计类型：病例对照研究
本次分析的主要目的：了解不同病某些共同症状的变化差异。
数据类型及变量的说明：y：病1，病2；X1：症状1（0/1）；……症状i（0/1）;X2：不同时间，day1....dayi
拟采用的分析方法：?。
主要存在的问题：版上讨论的计量RM资料分析较多，但对于计数资料(0,1);重复测量(day1-i)，该用什么方法怎么分析？此外，想知道不同时间的症状差异如何分析？
求助者email：minw@sohu.com
需要做脂肪代谢实验，打算通过在心肌新鲜组织匀浆中加入核素标记的脂肪酸代谢底物（[14C]-Palmitate），通过液体闪烁计数仪测定氧化产物[14C]CO2的放射性计数来反应脂肪酸的氧化代谢率。但是实验室只有γ放射免疫计数仪，请问能否用其测量“软β射线”14C；仪器需要作何调整吗？？？
定义：通过度量衡的方法，测量每一个观察单位的某项研究指标的量的大小，得到的一系列数据资料。
特点：★ 取值是定量的
★ 表现为数值大小
★ 有度量衡单位(计量单位)
★ 变量值是连续的
如：身高、红细胞计数、血压等
计数资料(enumerationdata)
定义：将全体观测单位按照某种性质或特征分组，然后再分别清点各组观察单位的个数。
特点：★ 取值是定性的(无度量衡单位计量单位)
★ 多为间断性资料
★ 数据分类互相排斥(互不相容)
★ 数据分类无逻辑顺序
★ 可分二项分类和多项分类
如：性别、血型等
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别告诉我计数的方法用数，我今天早上数了0.4g的微丸，近1000粒，快成熊猫，差点被送动物园了。也别告诉我测微丸的粒径用尺子量，我可是想着把它们排成一条线（增加准确度，可以避免忽略小粒子）再量，可是，这些小粒子不像《花园宝宝》里的小点点们那样听话，他们不爱排队。
各位老师是否还有什么高招？小的在这请教了。
