3-Aminobenzamide
Based on 8 publication(s) in Google Scholar
3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
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- 純度: 99.97%
- CAS 番号: 3544-24-9
- 分子式: C7H8N2O
- 分子量:136.15
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保管条件:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 3-Aminobenzamide
More- Acta Pharmacol Sin. 2023 Sep;44(9):1906-1919. [Abstract]
- Acta Pharmacol Sin. 2019 May;40(5):589-598. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Fish Shellfish Immunol. 2023 Apr:135:108682. [Abstract]
- Biochim Biophys Acta. 2016 Dec;1863(12):3027-3039. [Abstract]
- Mol Cell Endocrinol. 2018 Oct 15:474:137-150. [Abstract]
- J Cell Biochem. 2019 Apr;120(4):4813-4826. [Abstract]
- Patent. US20180263995A1.
Customer Validation & Images
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生物活性
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PARP 50 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| L1210 | IC50 |
19.1 μM
Compound: 3-Aminobenzamide
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Inhibition of the DNA repair Poly (ADP-ribose) polymerase 1, in permeabilised L1210 murine leukemia cells
Inhibition of the DNA repair Poly (ADP-ribose) polymerase 1, in permeabilised L1210 murine leukemia cells
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[PMID: 9857092] |
3-Aminobenzamide (PARP-IN-1) (>1 μM) causes more than 95% inhibition of PARP activity without significant cellular toxicity. INO-1001 significantly sensitizes CHO cells by blocking most of the DNA repair occurring between radiation fractions[1]. 3-Aminobenzamide significantly improves endothelial function by enhancing the acetylcholine-induced, endothelium-dependent, nitric oxide mediated vasorelaxation after exposure with 400 μM H2O2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3544-24-9
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性状 Solid
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分子量 136.15
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分子式 C7H8N2O
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Color Off-white to light brown
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SMILES
O=C(C1=CC=CC(N)=C1)N
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別名
PARP-IN-1; 3-アミノベンズアミド
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
TAX1BP1 contributes to deoxypodophyllotoxin-induced glioma cell parthanatos via inducing nuclear translocation of AIF by activation of mitochondrial respiratory chain complex I. [Abstract]2023 Sep;44(9):1906-1919. PMID: 37186123 -
Acta Pharmacol Sin
PARP1 interacts with HMGB1 and promotes its nuclear export in pathological myocardial hypertrophy. [Abstract]2019 May;40(5):589-598. PMID: 30030529 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Fish Shellfish Immunol
Nano-selenium protects grass carp hepatocytes against 4-tert-butylphenol-induced mitochondrial apoptosis and necroptosis via suppressing ROS-PARP1 axis. [Abstract]2023 Apr:135:108682. PMID: 36924910 -
Biochim Biophys Acta
The poly(ADP-ribosyl)ation of FoxO3 mediated by PARP1 participates in isoproterenol-induced cardiac hypertrophy. [Abstract]2016 Dec;1863(12):3027-3039. PMID: 27686254
3-Aminobenzamide purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1863(12):3027-3039. [Abstract]
The protein expression of PAR and PARP1, FoxO3 and phosphorylated FoxO3 (T32, S252 and S314), and FoxO3 in the nucleus and cytoplasm is measured byWestern blotting. The results are normalized to those of α-tubulin/Lamin B1 and are presented as the means ± SEM.
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Mol Cell Endocrinol
PARP1 interacts with STAT3 and retains active phosphorylated-STAT3 in nucleus during pathological myocardial hypertrophy. [Abstract]2018 Oct 15:474:137-150. PMID: 29501586
3-Aminobenzamide purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2018 Oct 15:474:137-150. [Abstract]
Rat heart tissues, which are injected with Ad-PARP1 or treated with 3AB following AAC surgery, the nuclear fraction are immunoprecipitated with anti-PARP1 antibody and subsequently subjected to immunoblotting analysis. n=3.
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J Cell Biochem
Poly(ADP-ribose) polymerase 1 induces cardiac fibrosis by mediating mammalian target of rapamycin activity. [Abstract]2019 Apr;120(4):4813-4826. PMID: 29278652
3-Aminobenzamide purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Apr;120(4):4813-4826. [Abstract]
The protein expression of PARP1 and the phosphorylation levels of mTOR target substrates, including S6K1, 4E-BP, and ULK1, are partially reversed in the abdominal aortic constriction (AAC) model after treatment with 3AB or Rapamycin.
3-Aminobenzamide purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Apr;120(4):4813-4826. [Abstract]
3-Aminobenzamide (3AB; 10 uM) clearly attenuates the cardiac fibrosis triggered by TGF-β1, as demonstrated by the reduction in protein levels of FN and Col I .
3-Aminobenzamide purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Apr;120(4):4813-4826. [Abstract]
In the 3-Aminobenzamide (3AB) plus TGF-β1 group, the phosphorylation of target substrates of mTOR (S6K1 and 4E-BP) is conformably lower than TGF-β1 treatment, as shown by western blotting.
3-Aminobenzamide purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Apr;120(4):4813-4826. [Abstract]
In the 3-Aminobenzamide (3AB) plus TGF-β1 group, the phosphorylation of target substrates of mTOR (ULK1) is conformably lower than TGF-β1 treatment, as shown by western blotting.
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溶剤 & 溶解度
DMSO : 100 mg/mL (734.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 11.11 mg/mL (81.60 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (36.72 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (36.72 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 25 mg/mL (183.62 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Radovits T, et al. Poly(ADP-ribose) polymerase inhibition improves endothelial dysfunction induced by reactive oxidant hydrogen peroxide in vitro. Eur J Pharmacol. 2007 Jun 14;564(1-3):158-66. [Content Brief]
[3]. Szabo C, et al. Poly(ADP-ribose) polymerase inhibitors ameliorate nephropathy of type 2 diabetic Leprdb/db mice. Diabetes. 2006 Nov;55(11):3004-12. [Content Brief]
[4]. Clark RS, 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 Aug;24(8):1399-405. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 7.3448 mL | 36.7242 mL | 73.4484 mL | 183.6210 mL |
| 5 mM | 1.4690 mL | 7.3448 mL | 14.6897 mL | 36.7242 mL | |
| 10 mM | 0.7345 mL | 3.6724 mL | 7.3448 mL | 18.3621 mL | |
| 15 mM | 0.4897 mL | 2.4483 mL | 4.8966 mL | 12.2414 mL | |
| 20 mM | 0.3672 mL | 1.8362 mL | 3.6724 mL | 9.1811 mL | |
| 25 mM | 0.2938 mL | 1.4690 mL | 2.9379 mL | 7.3448 mL | |
| 30 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL | 6.1207 mL | |
| 40 mM | 0.1836 mL | 0.9181 mL | 1.8362 mL | 4.5905 mL | |
| 50 mM | 0.1469 mL | 0.7345 mL | 1.4690 mL | 3.6724 mL | |
| 60 mM | 0.1224 mL | 0.6121 mL | 1.2241 mL | 3.0604 mL | |
| 80 mM | 0.0918 mL | 0.4591 mL | 0.9181 mL | 2.2953 mL | |
| DMSO | 100 mM | 0.0734 mL | 0.3672 mL | 0.7345 mL | 1.8362 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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