INO-1001
(Synonyms: 3-氨基苯甲酰胺,3-aminobenzamide) 目录号 : GC12496
A PARP inhibitor
Cas No.:3544-24-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Kinase experiment: |
PARP activity is measured with a PARP Activity Assay Kit. This method measures relative PARP activity by determining the level of incorporation of 3H-NAD into trichloroacetic acid (TCA) precipitable material in the presence of sheared genomic DNA, which activates PARP. The reaction mixture is added directly to washed cultures in 12-well culture plates and the reaction is allowed to proceed for 60 minutes at 37°C before the cells are removed mechanically, transferred to a microcentrifuge tube, and precipitated with ice-cold 5% TCA. |
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Animal experiment: |
Male db/db (Leprdb/db) mice, together with nondiabetic control db/m mice on C57BLKs/J background, are used. INO-1001 and PJ-34 treatment are initiated at 5 weeks of age. In sterile water that is sweetened with NutraSweet, 4.8 g/L 3-Aminobenzamide and 2.4 g/L PJ-34 is dissolved. Control animals receive sweetened water only. The average inhibitor consumption is 60 mg/kg 3-Aminobenzamide and 30 mg/kg PJ-34. |
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References: [1]. Brock WA, et al. Radiosensitization of human and rodent cell lines by INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase. Cancer Lett. 2004 Mar 18;205(2):155-60. |
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INO-1001 is a potent and selective inhibitor of PARP [1].
Poly(ADP-ribose) polymerase (PARP) is an enzyme involved in DNA repair and as a mediator of energy failure-induced cell death and NAD+ depletion [1].
In rodent and human fibroblast cell lines, INO-1001 significantly inhibited PARP activity. Treatment of 10 μM INO-1001 and a single dose of radiation caused significant radiosensitization of the three cells lines. While apoptosis was not increased, suggesting that INO-1001 increased radiation-induced cell killing through interfering with DNA repair mechanisms, increasing necrotic cell death [2].
In adult male mice subjected to moderate controlled cortical impact (CCI), injection intracerebral with INO-1001 (1.6 mg/kg) preserved brain NAD+ levels. In the Morris water maze, INO-1001 reduced the latency time to find the hidden platform and increased the time in the target quadrant [1]. In dogs underwent hypothermic cardiopulmonary bypass, reperfusion for 60 min after treatment with INO-1001 (1 mg/kg), INO-1001 significantly recovered left and right ventricular systolic function, increased coronary blood flow [3].
References:
[1]. Clark RS, Vagni VA, Nathaniel PD, et al. Local administration of the poly(ADP-ribose) polymerase inhibitor INO-1001 prevents NAD+ depletion and improves water maze performance after traumatic brain injury in mice. J Neurotrauma, 2007, 24(8): 1399-1405.
[2]. Szabó G, Soós P, Mandera S, et al. INO-1001 a novel poly(ADP-ribose) polymerase (PARP) inhibitor improves cardiac and pulmonary function after crystalloid cardioplegia and extracorporal circulation. Shock, 2004, 21(5): 426-432.
[3]. Brock WA, Milas L, Bergh S, et al. Radiosensitization of human and rodent cell lines by INO-1001, a novel inhibitor of poly(ADP-ribose) polymerase. Cancer Lett, 2004, 205(2): 155-160.
| Cas No. | 3544-24-9 | SDF | |
| 别名 | 3-氨基苯甲酰胺,3-aminobenzamide | ||
| 化学名 | 3-aminobenzamide | ||
| Canonical SMILES | C1=CC(=CC(=C1)N)C(=O)N | ||
| 分子式 | C7H8N2O | 分子量 | 136.15 |
| 溶解度 | Buffer: 30 mg/ml,DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 2 mg/ml | 储存条件 | Store at RT |
| 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 | 7.3448 mL | 36.7242 mL | 73.4484 mL |
| 5 mM | 1.469 mL | 7.3448 mL | 14.6897 mL |
| 10 mM | 0.7345 mL | 3.6724 mL | 7.3448 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。