PARP-1-IN-2
Based on 1 Customer Validation
PARP-1-IN-2 (compound 11g) is a potent PARP1 inhibitor, with an IC50 of 149 nM, and ADME prediction indicates it has high blood-brain barrier permeability. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 684234-55-7
- Formula: C22H15Cl2N3O2
- Molecular Weight:424.28
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Pyroptosis Compound Library
HY-L059
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
MCE Bioactive Compound Library
HY-L001V
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
All Caspase Isoforms
More
Biological Activity
|
PARP-1 149 ± 11.0 nM (IC50) |
Caspase-3 |
Caspase-9 |
PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells[1].
PARP-1-IN-2 (0-10 μM, 24 h) decreases the expression of pro-caspase-3 and phosphorylated AKT, increases the expression of caspase-3, caspase-9 protein and the cleaved PARP-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549, HFF cells[1]
-
Concentration:0, 0.1, 1, 10 μM
-
Incubation Time:24, 48 h
-
Result:Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells.
-
Cell Line:A549 cells[1]
-
Concentration:0, 0.1, 1, 10 μM
-
Incubation Time:24 h
-
Result:Reduced expression of pro-caspase-3 and phosphorylated AKT, significantly increased the expression of caspase-3 and caspase-9 protein, and enhanced expression of the cleaved PARP-1.
Chemical Information
-
CAS No. 684234-55-7
-
Appearance Solid
-
Molecular Weight 424.28
-
Formula C22H15Cl2N3O2
-
Color White to off-white
-
SMILES
O=C(NC1=CC=CC(Cl)=C1)CN(N=C(C2=CC=C(Cl)C=C2)C3=C4C=CC=C3)C4=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 83.33 mg/mL (196.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.90 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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 (protect from light)
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
-
Data Sheet (275 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3569 mL | 11.7847 mL | 23.5693 mL | 58.9234 mL |
| 5 mM | 0.4714 mL | 2.3569 mL | 4.7139 mL | 11.7847 mL | |
| 10 mM | 0.2357 mL | 1.1785 mL | 2.3569 mL | 5.8923 mL | |
| 15 mM | 0.1571 mL | 0.7856 mL | 1.5713 mL | 3.9282 mL | |
| 20 mM | 0.1178 mL | 0.5892 mL | 1.1785 mL | 2.9462 mL | |
| 25 mM | 0.0943 mL | 0.4714 mL | 0.9428 mL | 2.3569 mL | |
| 30 mM | 0.0786 mL | 0.3928 mL | 0.7856 mL | 1.9641 mL | |
| 40 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4731 mL | |
| 50 mM | 0.0471 mL | 0.2357 mL | 0.4714 mL | 1.1785 mL | |
| 60 mM | 0.0393 mL | 0.1964 mL | 0.3928 mL | 0.9821 mL | |
| 80 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2357 mL | 0.5892 mL |
PARP-1-IN-2 Related Classifications
HY-147027 Related Classifications
Powered by Bioz