PROTAC Sirt2 Degrader-2
Based on 1 Customer Validation
PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer.
(Pink: SIRT3 ligand (HY-19339); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-B0236)).
For research use only. We do not sell to patients.
- Purity : 98.05%
- CAS No.: 3123329-68-7
- Formula: C37H42N6O5S
- Molecular Weight:682.83
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
SIRT2 |
Cereblon |
In Vitro
PROTAC Sirt2 Degrader-2 (Compound W10) (72 h) exhibits potent antiproliferative activity and high selectivity against various ovarian cancer cell lines, including SKOV3 (IC50 = 0.33 μM), OVCAR3 (IC50 = 0.25 μM), and A2780 (IC50 = 0.08 μM) ovarian cancer cells, while showing lower toxicity against normal cells IOSE80 (CC50 = 2.64 μM)[1].
PROTAC Sirt2 Degrader-2 (0.01-20 μM, 6-48 h) efficiently and selectively degrades SIRT2 protein in A2780 ovarian cancer cells. The mechanism is concentration- and time-dependent, but a hook effect occurs at high concentrations[1].
PROTAC Sirt2 Degrader-2 (1 h) increases the thermal stability of the SIRT2 protein in A2780 ovarian cancer cells, indicating that PROTAC Sirt2 Degrader-2 directly binds to SIRT2 and stabilizes its structure[1].
PROTAC Sirt2 Degrader-2 (0.01-5 μM, 14 days) inhibits colony formation in A2780 cells in a concentration-dependent manner[1].
PROTAC Sirt2 Degrader-2 (0.01-10 μM, 36 h) induces cell cycle arrest in A2780 cells during the S and G2/M phases[1].
PROTAC Sirt2 Degrader-2 (0.01-10 μM, 36 h) induces early and late apoptosis in A2780 cells in a concentration-dependent manner, with late apoptosis being more significant[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780 ovarian cancer cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM
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Incubation Time:6 h, 9 h, 12 h, 24 h, 36 h, 48 h
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Result:Degradation was concentration-dependent (effective at 0.01 μmol/L, optimal at 1 μM, and exhibited a hook effect at 20 μM).
Degradation was time-dependent (significant effect after 36 hours).
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Cell Line:A2780 ovarian cancer cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:36 h
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Result:Induced cell cycle arrest in A2780 cells during the S and G2/M phases.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5 × 106 cells human ovarian cancer cell line A2780 were injected subcutaneously into the right axillary region of female BALB/c nude mice (4 weeks old)[1].
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Dosage:3 mg/kg, 5 mg/kg, 10 mg/kg
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Administration:I.p., once every two days
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Result:Significantly inhibited the growth of ovarian cancer xenografts.
Mice maintained stable body weight.
Effectively degraded SIRT2 protein in vivo.
The proportion of Ki-67 positive cells was significantly reduced, indicating that tumor cell proliferation was inhibited.
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Cell migration
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Protocol for Kinase activity and phosphorylation assays
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3123329-68-7
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Appearance Solid
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Molecular Weight 682.83
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Formula C37H42N6O5S
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Color White to off-white
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SMILES
CC(C)(C)C1=CC=C(C(NC(NC2=CC=C(NC(CCCCCNC3=C(CN(C4C(NC(CC4)=O)=O)C5=O)C5=CC=C3)=O)C=C2)=S)=O)C=C1
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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 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (146.45 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. 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)
In Vivo:
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 (3.66 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.
In Vivo Dissolution Calculator
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 (280 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. 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 |
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| DMSO | 1 mM | 1.4645 mL | 7.3225 mL | 14.6449 mL | 36.6123 mL |
| 5 mM | 0.2929 mL | 1.4645 mL | 2.9290 mL | 7.3225 mL | |
| 10 mM | 0.1464 mL | 0.7322 mL | 1.4645 mL | 3.6612 mL | |
| 15 mM | 0.0976 mL | 0.4882 mL | 0.9763 mL | 2.4408 mL | |
| 20 mM | 0.0732 mL | 0.3661 mL | 0.7322 mL | 1.8306 mL | |
| 25 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4645 mL | |
| 30 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2204 mL | |
| 40 mM | 0.0366 mL | 0.1831 mL | 0.3661 mL | 0.9153 mL | |
| 50 mM | 0.0293 mL | 0.1464 mL | 0.2929 mL | 0.7322 mL | |
| 60 mM | 0.0244 mL | 0.1220 mL | 0.2441 mL | 0.6102 mL | |
| 80 mM | 0.0183 mL | 0.0915 mL | 0.1831 mL | 0.4577 mL | |
| 100 mM | 0.0146 mL | 0.0732 mL | 0.1464 mL | 0.3661 mL |
PROTAC Sirt2 Degrader-2 Related Classifications
HY-179388 Related Classifications
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