Didox
(Synonyms: 3,4-二羟基苯甲羟肟酸,NSC-324360) 目录号 : GC12266
Antioxidant and ribonucleotide reductase inhibitor
Cas No.:69839-83-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | RAW264.7 macrophages are treated with Didox alone, with 0.1 μg/mL LPS, or the two in combination. Cellular respiration, as an indication of cytotoxicity, is measured by the MTT assay, which quantifies mitochondrial dehydrogenase activity. Macrophages are plated into 96 well Costar plates at 105 cells per well in 100 μL of DMEM media. After 4 h of incubation at 37°C for adherence, compounds and DMSO carrier control (0.01% final) are added in triplicate over serial dilutions beginning with 200 μM per well in a total volume of 200 μL, and the plates incubated for 24 h. Four h before termination of the assay, each well receives 20 μL of a 5 mg/mL MTT solution in un-supplemented DMEM. After centrifugation, the supernatant for each well is discarded and cells containing reduced MTT are solubilized with 100 μL of acidified isopropanol (4 mM HCl, 0.1% NP-40 in isopropanol). Following a brief period of shaking, the optical density (O.D.) for each well is recorded at 550 nm. Each experiment is repeated three times and the data averaged from each triplicate, then expressed as percentage of the control O.D. values for each experiment[1]. |
Animal experiment: | Mice[2]Luciferase-tagged leukemia cells are transplanted into 8- week old, sublethally irradiated (4.5 Gy) C57Bl/6 mice by tail vein injection of 1.0×106 cells per mouse. Mice are injected with 150 mg/kg D-Luciferin, anesthetised with Isoflurane, and imaged using the IVIS 100 imaging system. Mice begin treatment with Didox upon detection of clear signal. The animals are treated with daily administrations of Didox (NSC-324360) at 425 mg/kg Didox by intraperitoneal injection (IP) for 5 days. Control animals receive 5% dextrose water by IP injection. Repeat imaging is performed on the day following the final treatment[2]. |
References: [1]. Matsebatlela TM, et al. 3,4-Dihydroxy-benzohydroxamic acid (Didox) suppresses pro-inflammatory profiles and oxidative stress in TLR4-activated RAW264.7 murine macrophages. Chem Biol Interact. 2015 May 25;233:95-105. | |
Didox is a synthetic antioxidant.
Polyhydroxylated aromatic compounds, both natural and synthetic, are important biological antioxidants.
In vitro: In a previous study, the brain tissue from patients with HIV encephalitis was immunostained for lipid peroxidation. The presence of oxidized proteins in the CSF and CSF-induced progressive decrease in mitochondrial activity correlated with the severity of cognitive impairment. Didox together with L-deprenyl, imidate, diosgenin, and ebselen could block the CSF-induced toxicity. No effect of trimidox, ruthenium red, or Quercetin was seen [1]. Another study found that the exposure of didox prior or post to radiation in both PC-3/vector and PC-3/Bcl-2 transfectants led to an increase in radiation enhancement ratios. A significant reduction in G(2)M phase was observed in cells exposed to didox post IR when compared to cells exposed to IR alone. In addition, the exposure to didox after radiation in PC-3/vector significantly abrogated radiation-induced Bcl-2 upregulation [2].
In vivo: In syngeneic, therapy-resistant AML models, single agent didox treatment led to a significant reduction in leukemia burden and a survival benefit. Didox was well tolerated and didox exposure at levels that impaired leukemia growth did not inhibit normal HSC engraftment [3].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Turchan, J. ,Pocernich, C.B.,Gairola, C., et al. Oxidative stress in HIV demented patients and protection ex vivo with novel antioxidants. Neurology 60, 307-314 (2003).
[2] Inayat, M. S.,Chendil, D.,Mohiuddin, M., et al. Didox (A novel ribonucleotide reductase inhibitor) Overcomes bcl-2 mediated radiation resistance in prostate cancer cell line PC-3. Cancer Biology and Therapy 1(5), 539-545 (2002).
[3] Cook GJ, Caudell DL, Elford HL, Pardee TS. The efficacy of the ribonucleotide reductase inhibitor Didox in preclinical models of AML. PLoS One. 2014 Nov 17;9(11):e112619.
| Cas No. | 69839-83-4 | SDF | |
| 别名 | 3,4-二羟基苯甲羟肟酸,NSC-324360 | ||
| 化学名 | N-3,4-tridhydroxy-benzamide | ||
| Canonical SMILES | ONC(=O)c1ccc(O)c(O)c1 | ||
| 分子式 | C7H7NO4 | 分子量 | 169.1 |
| 溶解度 | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | 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 | 5.9137 mL | 29.5683 mL | 59.1366 mL |
| 5 mM | 1.1827 mL | 5.9137 mL | 11.8273 mL |
| 10 mM | 0.5914 mL | 2.9568 mL | 5.9137 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。