Homocarbonyltopsentin
Based on 1 Customer Validation
Homocarbonyltopsentin (PK4C9) is a small-molecule TSL2-binding compound, binds to pentaloop conformations of TSL2 and promotes a shift to triloop conformations that display enhanced SMN2 exon 7 (E7) splicing with EC50 value of 16 μM.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 172286-77-0
- Formula: C21H14N4O3
- Molecular Weight:370.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
All DNA/RNA Synthesis Isoforms
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Biological Activity
Homocarbonyltopsentin (PK4C9) (10-40 μM; 24 hours) shows an up to 5.2-fold decrease in the expression of E7-excluding SMN2 isoforms, and up to three-fold increase in E7-including isoforms in GM03813C cells[1]. Homocarbonyltopsentin (PK4C9) (40 μM; 24 hours) increased 1.5-fold SMN protein expression compared to GM03813C cells treated with DMSO[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GM03813C (SMA) cells; GM03814B fibroblasts cells
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Concentration:10-40 μM
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Incubation Time:24 hours
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Result:E7 inclusion reached a maximum of 91% (25% increase, DMSO-treated cells).
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Cell Line:GM03813C (SMA) cells; GM03814B fibroblasts cells
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Concentration:40 μM
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Incubation Time:24 hours
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Result:Increased SMN protein in SMA cells.
Chemical Information
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CAS No. 172286-77-0
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Appearance Solid
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Molecular Weight 370.36
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Formula C21H14N4O3
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Color White to yellow
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SMILES
O=C(C1=NC=C(C(C2=CNC3=C2C=CC=C3)=O)N1)C4=CNC5=C4C=CC(O)=C5
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Synonyms
PK4C9
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (270.01 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, 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.
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.
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 (5.62 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.
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.
Purity & Documentation
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Data Sheet (274 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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7001 mL | 13.5004 mL | 27.0008 mL | 67.5019 mL |
| 5 mM | 0.5400 mL | 2.7001 mL | 5.4002 mL | 13.5004 mL | |
| 10 mM | 0.2700 mL | 1.3500 mL | 2.7001 mL | 6.7502 mL | |
| 15 mM | 0.1800 mL | 0.9000 mL | 1.8001 mL | 4.5001 mL | |
| 20 mM | 0.1350 mL | 0.6750 mL | 1.3500 mL | 3.3751 mL | |
| 25 mM | 0.1080 mL | 0.5400 mL | 1.0800 mL | 2.7001 mL | |
| 30 mM | 0.0900 mL | 0.4500 mL | 0.9000 mL | 2.2501 mL | |
| 40 mM | 0.0675 mL | 0.3375 mL | 0.6750 mL | 1.6875 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5400 mL | 1.3500 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4500 mL | 1.1250 mL | |
| 80 mM | 0.0338 mL | 0.1688 mL | 0.3375 mL | 0.8438 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6750 mL |