AGK2

製品コードS7577 バッチS757702

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H13Cl2N3O2
分子量 434.27 CAS No. 304896-28-4
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 10 mg/mL (23.02 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. This compound protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. [1] It 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]

プロトコル(参考用のみ)

キナーゼアッセイ Fluorescent SIRT enzyme assays
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+. This compound is 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 --

参考

  • https://pubmed.ncbi.nlm.nih.gov/17588900/
  • https://pubmed.ncbi.nlm.nih.gov/22166219/
  • https://pubmed.ncbi.nlm.nih.gov/24259290/

カスタマーフィードバック

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 ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Sirtuin 2 exacerbates renal tubule injury and inflammation in diabetic mice via deacetylation of c-Jun/c-Fos [ Cell Mol Life Sci, 2025, 82(1):45] PubMed: 39833479
Identifying Age-Modulating Compounds Using a Novel Computational Framework for Evaluating Transcriptional Age [ Aging Cell, 2025, e70075] PubMed: 40307992
SIRT2-dependent CPT1A deacetylation in macrophages inhibits periodontitis [ Front Pharmacol, 2025, 16:1574141] PubMed: 40606607
INHIBITING SIRT2 ATTENUATES SEPSIS-INDUCED ACUTE KIDNEY INJURY VIA FOXO1 ACETYLATION-MEDIATED AUTOPHAGY ACTIVATION [ Shock, 2025, 63(2):255-266] PubMed: 39527461
NAD+ precursors promote the restoration of spermatogenesis in busulfan-treated mice through inhibiting Sirt2-regulated ferroptosis [ Theranostics, 2024, 14(6):2622-2636] PubMed: 38646657
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
The SIRT2-AMPK axis regulates autophagy induced by acute liver failure [ Sci Rep, 2024, 14(1):16278] PubMed: 39009648
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

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。

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