PROTAC Sirt2 Degrader-1
Based on 1 publication(s) in Google Scholar
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
(Pink: SIRT2 ligand (HY-107453); Blue: Cereblon ligand (HY-103596); Black: linker (HY-184534)).
For research use only. We do not sell to patients.
- Purity: 99.09%
- CAS No.: 2098487-75-1
- Formula: C40H40N10O8S2
- Molecular Weight:852.94
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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) PROTAC Sirt2 Degrader-1
MoreAll PROTACs Isoforms
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Biological Activity
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SIRT2 0.25 μM (IC50) |
PROTAC Sirt2 Degrader-1 (Compound 12; 10 μM, 1-6 hours) induces Sirt2 degradation in HeLa cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:10 µM
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Incubation Time:1-6 hours
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Result:Caused Sirt2 degradation, but showed no effect on Sirt1 levels.
Chemical Information
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CAS No. 2098487-75-1
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Appearance Solid
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Molecular Weight 852.94
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Formula C40H40N10O8S2
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Color White to off-white
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SMILES
O=C(N(C(CCC1=O)C(N1)=O)C2=O)C(C2=CC=C3)=C3OCC(NCCCCN4C=C(COC5=CC(CC6=CN=C(NC(CSC7=NC(C)=CC(C)=N7)=O)S6)=CC=C5)N=N4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Solvent & Solubility
DMSO : ≥ 100 mg/mL (117.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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, 6 months; -20°C, 1 month. 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. 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (272 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)
- 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. 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 | 1.1724 mL | 5.8621 mL | 11.7242 mL | 29.3104 mL |
| 5 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8621 mL | |
| 10 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9310 mL | |
| 15 mM | 0.0782 mL | 0.3908 mL | 0.7816 mL | 1.9540 mL | |
| 20 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4655 mL | |
| 25 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1724 mL | |
| 30 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9770 mL | |
| 40 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 50 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL | |
| 60 mM | 0.0195 mL | 0.0977 mL | 0.1954 mL | 0.4885 mL | |
| 80 mM | 0.0147 mL | 0.0733 mL | 0.1466 mL | 0.3664 mL | |
| 100 mM | 0.0117 mL | 0.0586 mL | 0.1172 mL | 0.2931 mL |
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