受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H13Cl2N3O2 |
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分子量 | 434.27 | CAS No. | 304896-28-4 | |
Solubility (25°C)* | 体外 | DMSO | 4 mg/mL warmed with 50ºC water bath (9.21 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels. |
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in vitro | In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. AGK2 protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. [1] AGK2 induces both necrosis and caspase-3-dependent apoptosis in C6 glioma cells. [2] SIRT2 also decreases merlin-mutant viability of mouse schwann cells (MSCs) without substantially reducing wild-type MSC viability. [3] |
in vivo | In drosophila model of parkinson's disease, AGK2 rescues α-Syn–mediated toxicity and modify aggregation. [1] |
キナーゼアッセイ | Fluorescent SIRT enzyme assays | |
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Recombinant SIRT enzymes and fluorescent peptide substrates are used according to the manufacturer’s instructions. Briefly, substrate is added to a final concentration of 50 μM, supplemented with 500 μM NAD+. Compounds are then added to the appropriate wells, with controls receiving DMSO only. Finally, enzyme is added and the reaction allowed to proceed for 1 hr at 37°C, at which time a developer solution is added and the samples read at 355/460 nm. For the enzyme immunoprecipitation experiments, the procedure is the same as above except immunoprecipitated enzyme was used in place of recombinant enzyme. | ||
動物実験 | 動物モデル | Drosophila model of parkinson |
投薬量 | 1mM | |
投与方法 | -- |
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Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 46(2):451-460]
Data from [Data independently produced by , , Mol Cancer Res, 2018, doi:10.1158/1541-7786.MCR-18-0637]
Data from [Data independently produced by , , J Biol Chem, 2014, 289(9): 6054-66 ]
Mitochondrial aldehyde dehydrogenase-2 coordinates the hydrogen sulfide - AMPK axis to attenuate high glucose-induced pancreatic β-cell dysfunction by glutathione antioxidant system [ Redox Biol, 2024, 69:102994] | PubMed: 38128451 |
SIRT2 inhibition protects against cardiac hypertrophy and ischemic injury [ Elife, 2023, 12e85571] | PubMed: 37728319 |
SIRT2 inhibition protects against cardiac hypertrophy and ischemic injury [ Elife, 2023, 12e85571] | PubMed: 37728319 |
SIRT2 Inhibition Rescues Neurodegenerative Pathology but Increases Systemic Inflammation in a Transgenic Mouse Model of Alzheimer's Disease [ J Neuroimmune Pharmacol, 2023, 18(3):529-550] | PubMed: 37698780 |
Continuous Fluorescent Sirtuin Activity Assay Based on Fatty Acylated Lysines [ Int J Mol Sci, 2023, 24(8)7416] | PubMed: 37108579 |
VRK1 Kinase Activity Modulating Histone H4K16 Acetylation Inhibited by SIRT2 and VRK-IN-1 [ Int J Mol Sci, 2023, 24(5)4912] | PubMed: 36902348 |
High-Content and High-Throughput Clonogenic Survival Assay Using Fluorescence Barcoding [ Cancers -Basel), 2023, 15(19)4772] | PubMed: 37835466 |
AGK2 pre-treatment protects against thioacetamide-induced acute liver failure via regulating the MFN2-PERK axis and ferroptosis signaling pathway [ Hepatobiliary Pancreat Dis Int, 2023, S1499-3872(23)00037-1] | PubMed: 36966125 |
Regulation of reverse electron transfer at mitochondrial complex I by unconventional Notch action in cancer stem cells [ Dev Cell, 2022, 57(2):260-276.e9] | PubMed: 35077680 |
Arylamine N-Acetyltransferase 1 Activity is Regulated by the Protein Acetylation Status [ Front Pharmacol, 2022, 13:797469] | PubMed: 35153780 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。