SirReal2
Based on 2 publication(s) in Google Scholar
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration.
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- Purity: 99.0%
- CAS No.: 709002-46-0
- 화학식: C22H20N4OS2
- 분자량:420.55
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보관:Powder -20°C, 3 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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
HY-L005
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Immunology/Inflammation Compound Library
HY-L007
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Antioxidant Compound Library
HY-L037
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Reprogramming Compound Library
HY-L039
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Oxygen Sensing Compound Library
HY-L045
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Glutamine Metabolism Compound Library
HY-L064
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Anti-Blood Cancer Compound Library
HY-L079
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Anti-Hematopathy Compound Library
HY-L171
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Radioprotector Library
HY-L178
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Bioactive Compound Library Max
HY-L181
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Epigenetics Compound Library Mini
HY-L005M
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) SirReal2
More
Biological Activity
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SIRT2 140 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| K562 | IC50 |
>100 μM
Compound: SirReal2
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Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 1 day by MTT assay
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 1 day by MTT assay
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[PMID: 30885568] |
| MCF7 | IC50 |
13.7 μM
Compound: SirReal2
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 4 days by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 4 days by MTT assay
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[PMID: 30885568] |
| MT2 | IC50 |
>100 μM
Compound: SirReal2
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Cytotoxicity against human MT2 cells assessed as reduction in cell viability measured after 1 day by MTT assay
Cytotoxicity against human MT2 cells assessed as reduction in cell viability measured after 1 day by MTT assay
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[PMID: 30885568] |
SirReal2 (1 μM, 24 h) combined with VS-5584 (1μM, 24 h) inhibits acute myeloid leukemia cell proliferation, increases the proportion of apoptotic cells and induces cell cycle arrest[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SirReal2 (50 mg/kg, i.p., every 3 days for 19 days) inhibits the expression of SIRT2, resumes NK cell tumor infltration and suppresses melanoma progression in WT mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:mouse tumor xenograft model[3]
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Dosage:4 mg/kg
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Administration:i.p., every 3 days for 28 days
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Result:Restrained the growth of subcutaneous xenografts combined with VS-5584 in vivo.
Chemical Information
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CAS No. 709002-46-0
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Appearance Solid
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분자량 420.55
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화학식 C22H20N4OS2
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Color Off-white to light yellow
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SMILES
O=C(NC1=NC=C(CC2=C3C=CC=CC3=CC=C2)S1)CSC4=NC(C)=CC(C)=N4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 31.25 mg/mL (74.31 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)
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 (4.95 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 (4.95 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.
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.
순도&문서
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Data Sheet (276 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Rumpf T, et al. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site. Nat Commun. 2015 Feb 12;6:6263. [Content Brief]
[2]. Schiedel M, et al. Structure-Based Development of an Affinity Probe for Sirtuin 2. Angew Chem Int Ed Engl. 2016;55(6):2252-2256. [Content Brief]
[3]. Luo Y, et al. SIRT2 inhibitor SirReal2 enhances anti-tumor effects of PI3K/mTOR inhibitor VS-5584 on acute myeloid leukemia cells. Cancer Med. 2023 Sep;12(18):18901-18917. [Content Brief]
[4]. Zhang M, et al. SIRT2 promotes murine melanoma progression through natural killer cell inhibition. Sci Rep. 2021 Jun 21;11(1):12988. [Content Brief]
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 | 2.3778 mL | 11.8892 mL | 23.7784 mL | 59.4460 mL |
| 5 mM | 0.4756 mL | 2.3778 mL | 4.7557 mL | 11.8892 mL | |
| 10 mM | 0.2378 mL | 1.1889 mL | 2.3778 mL | 5.9446 mL | |
| 15 mM | 0.1585 mL | 0.7926 mL | 1.5852 mL | 3.9631 mL | |
| 20 mM | 0.1189 mL | 0.5945 mL | 1.1889 mL | 2.9723 mL | |
| 25 mM | 0.0951 mL | 0.4756 mL | 0.9511 mL | 2.3778 mL | |
| 30 mM | 0.0793 mL | 0.3963 mL | 0.7926 mL | 1.9815 mL | |
| 40 mM | 0.0594 mL | 0.2972 mL | 0.5945 mL | 1.4861 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1889 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9908 mL |
SirReal2 Related Classifications
HY-100591 Related Classifications
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