Quinoclamine
(Synonyms: 灭藻醌) 目录号 : GC39428
Quinoclamine 是一种萘醌衍生物，是一种 NF-κB 抑制剂。Quinoclamine 具有抗肿瘤活性。
Cas No.:2797-51-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Quinoclamine, a naphthoquinone derivative, is a NF-κB inhibitor. Quinoclamine exhibits anti-cancer activity[1][2].
[1]. Kwon H ,et al. Induction of differentiation of U-937 cells by 2-chloro-3-amino-1,4-naphthoquinone. Res Commun Mol Pathol Pharmacol. 1997 Aug;97(2):215-27. [2]. Cheng WY, et al. Comprehensive evaluation of a novel nuclear factor-kappaB inhibitor, quinoclamine, by transcriptomic analysis. Br J Pharmacol. 2009 Jul;157(5):746-56.
| Cas No. | 2797-51-5 | SDF | |
| 别名 | 灭藻醌 | ||
| Canonical SMILES | O=C(C(Cl)=C(C1=O)N)C2=C1C=CC=C2 | ||
| 分子式 | C10H6ClNO2 | 分子量 | 207.61 |
| 溶解度 | DMSO: 250 mg/mL (1204.18 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8167 mL | 24.0836 mL | 48.1672 mL |
| 5 mM | 0.9633 mL | 4.8167 mL | 9.6334 mL |
| 10 mM | 0.4817 mL | 2.4084 mL | 4.8167 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Comprehensive evaluation of a novel nuclear factor-kappaB inhibitor, Quinoclamine, by transcriptomic analysis
Br J Pharmacol 2009 Jul;157(5):746-56.PMID:19422389DOI:10.1111/j.1476-5381.2009.00223.x.
Background and purpose: The transcription factor nuclear factor-kappaB (NF-kappaB) has been linked to the cell growth, apoptosis and cell cycle progression. NF-kappaB blockade induces apoptosis of cancer cells. Therefore, NF-kappaB is suggested as a potential therapeutic target for cancer. Here, we have evaluated the anti-cancer potential of a novel NF-kappaB inhibitor, Quinoclamine (2-amino-3-chloro-1,4-naphthoquinone). Experimental approach: In a large-scale screening test, we found that Quinoclamine was a novel NF-kappaB inhibitor. The global transcriptional profiling of Quinoclamine in HepG2 cells was therefore analysed by transcriptomic tools in this study. Key results: Quinoclamine suppressed endogenous NF-kappaB activity in HepG2 cells through the inhibition of IkappaB-alpha phosphorylation and p65 translocation. Quinoclamine also inhibited induced NF-kappaB activities in lung and breast cancer cell lines. Quinoclamine-regulated genes interacted with NF-kappaB or its downstream genes by network analysis. Quinoclamine affected the expression levels of genes involved in cell cycle or apoptosis, suggesting that Quinoclamine exhibited anti-cancer potential. Furthermore, Quinoclamine down-regulated the expressions of UDP glucuronosyltransferase genes involved in phase II drug metabolism, suggesting that Quinoclamine might interfere with drug metabolism by slowing down the excretion of drugs. Conclusion and implications: This study provides a comprehensive evaluation of Quinoclamine by transcriptomic analysis. Our findings suggest that Quinoclamine is a novel NF-kappaB inhibitor with anti-cancer potential.
Combined exposure to low doses of pesticides causes decreased birth weights in rats
Reprod Toxicol 2017 Sep;72:97-105.PMID:28526456DOI:10.1016/j.reprotox.2017.05.004.
Decreased birth weight is a common effect of many pesticides in reproductive toxicity studies, but there are no empirical data on how pesticides act in combination on this endpoint. We hypothesized that a mixture of six pesticides (cyromazine, MCPB, pirimicarb, Quinoclamine, thiram, and ziram) would decrease birth weight, and that these mixture effects could be predicted by the Dose Addition model. Data for the predictions were obtained from the Draft Assessment Reports of the individual pesticides. A mixture of equi-effective doses of these pesticides was tested in two studies in Wistar rats, showing mixture effects in good agreement with the additivity predictions. Significantly lower birth weights were observed when compounds were present at individual doses below their no-observed adverse effect levels (NOAELs). These results emphasize the need for cumulative risk assessment of pesticides to avoid potentially serious impact of mixed exposure on prenatal development and pregnancy in humans.
Effects of five rice herbicides on the growth of two threatened aquatic ferns
Ecotoxicol Environ Saf 2006 Mar;63(3):463-8.PMID:16406589DOI:10.1016/j.ecoenv.2005.02.010.
The effects of five rice herbicides bensulfuron methyl, mefenacet, Quinoclamine, simetryn, and thiobencarb on the growth of two threatened aquatic ferns Azolla japonica and Salvinia natans were tested using 12-day exposure experiments at 0.1-100 nM which are expected to be present in drainages and rivers in Japan. As a reference species, Lenma minor was also used to examine the toxicity of bensulfuron methyl. Bensulfuron methyl had the most pronounced effect on the relative growth rate (RGR) of A. japonica, S. natans, and L. minor with an EC50 of 5.0, 0.54, and 10 nM, respectively. The other herbicides reduced the RGR of the aquatic ferns only at the highest concentration (100 nM) or not at all. S. natans showed the highest susceptibility to bensulfuron methyl among the three species, and the EC50 for this species was comparable to or below the maximum concentration (0.49-5.6 nM) that had been previously detected in 7 of 11 rivers in Japan. These results suggest that bensulfuron methyl runoff in drainages and rivers in Japan is expected to have adverse effects on the growth of threatened aquatic ferns in some cases, and that no or small effects occur for the other four herbicides tested.
Effects of four rice paddy herbicides on algal cell viability and the relationship with population recovery
Environ Toxicol Chem 2011 Aug;30(8):1898-905.PMID:21590715DOI:10.1002/etc.582.
Paddy herbicides are a high-risk concern for aquatic plants, including algae, because they easily flow out from paddy fields into rivers, with toxic effects. The effect on algal population dynamics, including population recovery after timed exposure, must be assessed. Therefore, we demonstrated concentration-response relationships of four paddy herbicides for algal growth inhibition and mortality, and the relationship between the effect on algal cell viability and population recovery following exposure. We used SYTOX Green dye assay and flow cytometry to assess cell viability of the alga Pseudokirchneriella subcapitata. Live cells could be clearly distinguished from dead cells during herbicide exposure. Our results showed that pretilachlor and Quinoclamine had both algicidal and algistatic effects, whereas bensulfuron-methyl only had an algistatic effect, and pentoxazone only had an algicidal effect. Then, a population recovery test following a 72-h exposure was conducted. The algal population recovered in all tests, but the periods required for recovery differed among exposure concentrations and herbicides. The periods required for recovery were inconsistent with the dead cell ratio at the beginning of the recovery test; that is, population recovery could not be described only by cell viability. Consequently, the temporal effect of herbicides and subsequent recovery of the algal population could be described not only by the toxicity characteristics but also by toxicokinetics, such as rate of uptake, transport to the target site, and elimination of the substance from algal cells.
Effects on metabolic parameters in young rats born with low birth weight after exposure to a mixture of pesticides
Sci Rep 2018 Jan 10;8(1):305.PMID:29321614DOI:10.1038/s41598-017-18626-x.
Pesticide exposure during fetal life can lead to low birth weight and is commonly observed in reproductive toxicology studies. Associations have also been found in low birth weight babies born from pesticide-exposed gardeners. Since low birth weight is also linked to metabolic disorders, it can be speculated that early life exposure to pesticides could increase the risk of becoming obese or developing diabetes later in life. We have analyzed potential long-term effects of gestational and lactational exposure to a low dose mixture of six pesticides that individually can cause low birth weight: Cyromazine, MCPB, Pirimicarb, Quinoclamine, Thiram, and Ziram. Exposed male offspring, who were smaller than controls, displayed some degree of catch-up growth. Insulin and glucagon regulation was not significantly affected, and analyses of liver and pancreas did not reveal obvious histopathological effects. Efforts towards identifying potential biomarkers of metabolic disease-risk did not result in any strong candidates, albeit leptin levels were altered in exposed animals. In fat tissues, the key genes Lep, Nmb and Nmbr were altered in high dosed offspring, and were differentially expressed between sexes. Our results suggest that early-life exposure to pesticides may contribute to the development of metabolic disorders later in life.