SIRT2-IN-11
Based on 1 Customer Validation
SIRT2-IN-11 (AEM1) is a selective SIRT2 inhibitor with an IC50 value of 18.5 μM. SIRT2-IN-11 p53-dependently induces apoptosis, activates expression of CDKN1A, PUMA and NOXA, and increases acetylation of p53. SIRT2-IN-11 can be used for the research of p53-related cancers.
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- 純度 : 99.94%
- CAS 番号: 1005095-06-6
- 分子式: C21H22N2O
- 分子量:318.41
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
製品説明
IC50 & Target
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SIRT2 18.5 μM (IC50) |
SIRT1 118.4 μM (IC50) |
体外実験
SIRT2-IN-11 (0-1000 μM) shows inhibitory effect of SIRT2-dependent deacetylation of MAL with an IC50 value of 18.5 μM[1]. SIRT2-IN-11 (0-1000 μM) weakly inhibits SIRT1 with an IC50 value of 118.4 μM[1]. SIRT2-IN-11 (0-20 μM; 8 h) induces cell apoptosis of lung cancer cells[1]. SIRT2-IN-11 (20 μM; 6 h) increases p53 acetylation and expression levels of Cp53 target genes CDKN1A, PUMA and NOXA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:NSCLC cell lines
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Concentration:20 μM
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Incubation Time:6 hours
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Result:Increased the expression of CDKN1A, PUMA and NOXA.
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Cell Line:A549 cell line
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Concentration:0, 0.5, 1, 5, 10 and 20 μM
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Incubation Time:24 hours
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Result:Mildly increased apoptosis of A549 cells, but when combined treatment with etoposide caused a marked increase in apoptosis.
化学情報
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CAS 番号 1005095-06-6
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性状 Solid
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分子量 318.41
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分子式 C21H22N2O
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Color White to off-white
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SMILES
O=C(C1=CC=C2NC(C3C(C4CCC3C4)C2=C1)C5=CC=CC=C5)N
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 250 mg/mL (785.15 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 3.1406 mL | 15.7030 mL | 31.4060 mL | 78.5151 mL |
| 5 mM | 0.6281 mL | 3.1406 mL | 6.2812 mL | 15.7030 mL | |
| 10 mM | 0.3141 mL | 1.5703 mL | 3.1406 mL | 7.8515 mL | |
| 15 mM | 0.2094 mL | 1.0469 mL | 2.0937 mL | 5.2343 mL | |
| 20 mM | 0.1570 mL | 0.7852 mL | 1.5703 mL | 3.9258 mL | |
| 25 mM | 0.1256 mL | 0.6281 mL | 1.2562 mL | 3.1406 mL | |
| 30 mM | 0.1047 mL | 0.5234 mL | 1.0469 mL | 2.6172 mL | |
| 40 mM | 0.0785 mL | 0.3926 mL | 0.7852 mL | 1.9629 mL | |
| 50 mM | 0.0628 mL | 0.3141 mL | 0.6281 mL | 1.5703 mL | |
| 60 mM | 0.0523 mL | 0.2617 mL | 0.5234 mL | 1.3086 mL | |
| 80 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9814 mL | |
| 100 mM | 0.0314 mL | 0.1570 mL | 0.3141 mL | 0.7852 mL |