PARP1-IN-5 dihydrochloride
Based on 1 publication(s) in Google Scholar
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 97.56%
- CAS No.: 2823308-89-8
- Formula: C25H26Cl2N2O5S
- Molecular Weight:537.46
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PARP1-IN-5 dihydrochloride
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Biological Activity
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PARP-1 14.7 nM (IC50) |
PARP-2 0.9 μM (IC50) |
PARP1-IN-5 dihydrochloride (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 dihydrochloride (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 dihydrochloride (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 dihydrochloride (SK-OV-3 cells) can significantly decrease the PAR level[1].
PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg[1].
PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 dihydrochloride can upregulate the expression of γ-H2AX and decrease the expression of PAR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:1000 mg/kg
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Administration:P.o.
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Result:There was no significant difference in the body weight and blood routine.
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Animal Model:Mice[1]
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Dosage:25 and 50 mg/kg
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Administration:P.o.; 12 days
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Result:Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.
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Animal Model:Male Sprague−Dawley (SD) rats[1]
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Dosage:50 mg/kg (Pharmacokinetic Analysis)
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Administration:P.o.
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Result:Positively correlated with the expression of PARP-1.
Chemical Information
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CAS No. 2823308-89-8
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Appearance Solid
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Molecular Weight 537.46
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Formula C25H26Cl2N2O5S
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Color Light yellow to green yellow
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SMILES
O=C1C=C(OC2=C1C(O)=CC(O)=C2CN3CCN(CC3)CC4=CC=CS4)C5=CC=C(C=C5)O.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Apoptosis
Excessive hydrogen sulfide causes lung and brain tissue damage by promoting PARP1/Bax and C9 and inhibiting LAMB1. [Abstract]2022 Feb;27(1-2):149-160. PMID: 35119561
Solvent & Solubility
DMSO : 125 mg/mL (232.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (1.86 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (3.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8606 mL | 9.3030 mL | 18.6060 mL | 46.5151 mL |
| DMSO | 5 mM | 0.3721 mL | 1.8606 mL | 3.7212 mL | 9.3030 mL |
| 10 mM | 0.1861 mL | 0.9303 mL | 1.8606 mL | 4.6515 mL | |
| 15 mM | 0.1240 mL | 0.6202 mL | 1.2404 mL | 3.1010 mL | |
| 20 mM | 0.0930 mL | 0.4652 mL | 0.9303 mL | 2.3258 mL | |
| 25 mM | 0.0744 mL | 0.3721 mL | 0.7442 mL | 1.8606 mL | |
| 30 mM | 0.0620 mL | 0.3101 mL | 0.6202 mL | 1.5505 mL | |
| 40 mM | 0.0465 mL | 0.2326 mL | 0.4652 mL | 1.1629 mL | |
| 50 mM | 0.0372 mL | 0.1861 mL | 0.3721 mL | 0.9303 mL | |
| 60 mM | 0.0310 mL | 0.1551 mL | 0.3101 mL | 0.7753 mL | |
| 80 mM | 0.0233 mL | 0.1163 mL | 0.2326 mL | 0.5814 mL | |
| 100 mM | 0.0186 mL | 0.0930 mL | 0.1861 mL | 0.4652 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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