SRT2104 (GSK2245840)

製品コードS7792 バッチS779202

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

C26H24N6O2S2
分子量 516.64 CAS No. 1093403-33-8
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 4 mg/mL (7.74 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 SRT2104 (GSK2245840)は、エネルギーホメオスタシスの調節に関与する選択的SIRT1活性化因子です。フェーズ2。
in vitro SRT2104 (GSK2245840) reduces p65/RelA acetylation levels in C2C12 cells.
in vivo In male C57BL/6J mice, SRT2104 (GSK2245840) (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard diet, enhances motor coordination, bone mineral density, and insulin sensitivity, and decreases inflammation. Short-term treatment with this compound preserves bone and muscle mass in an experimental model of atrophy. In Male N171-82Q HD mice, it (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival.

プロトコル(参考用のみ)

キナーゼアッセイ SIRT1 fluorescence polarization assay and HTS
In the SIRT1 FP assay for SRT2104 (GSK2245840), SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2 ) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD +, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2 , 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 ℃ in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths.
細胞アッセイ 細胞株 C2C12 cell line
濃度 3 μM
反応時間 24 h
実験の流れ Cells are cultured in low glucose Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum and penicillin–streptomycin. They are treated with vehicle (0.1% DMSO) or 3 μM SRT2104 (GSK2245840) for 24 h and then harvested for protein and Western blotting.
動物実験 動物モデル Male N171-82Q HD mice
投薬量 diet containing 0.5% SRT2104
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/24931715/
  • https://pubmed.ncbi.nlm.nih.gov/25574479/
  • https://pubmed.ncbi.nlm.nih.gov/18046409/

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：

Suppression of FOXO1 activity by SIRT1-mediated deacetylation weakening the intratumoral androgen autocrine function in glioblastoma [ Cancer Gene Ther, 2025, 32(3):343-354] PubMed: 40075208
Sodium tanshinone IIA sulfonate alleviates osteoarthritis through targeting SIRT1 [ Chin Med, 2025, 20(1):142] PubMed: 40890747
SRT2104 enhances dendritic outgrowth and spine formation through Sirtuin 1-mediated mTORC1 signaling [ Sci Rep, 2025, 15(1):21283] PubMed: 40594837
Upregulation of SIRT1 ameliorates apoptosis of rat nucleus pulposus cells under oxidative stress through FoxO1/β-catenin pathway [ Folia Histochem Cytobiol, 2025, 10.5603/fhc.104395] PubMed: 40421819
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] PubMed: 39264808
SIRT1 maintains bone homeostasis by regulating osteoblast glycolysis through GOT1 [ Cell Mol Life Sci, 2024, 81(1):204] PubMed: 38700532
MicroRNA-141-3p reduces pulmonary hypoxia/reoxygenation injury through suppression of Beclin-1-dependent autophagy [ Aging (Albany NY), 2024, 16(2):1352-1373] PubMed: 38261732
Activation of nemo-like kinase in diamond blackfan anemia suppresses early erythropoiesis by preventing mitochondrial biogenesis [ J Biol Chem, 2024, 300(8):107542] PubMed: 38992436
Neuroprotection of SRT2104 in Murine Ischemia/Reperfusion Injury Through the Enhancement of Sirt1-Mediated Deacetylation [ Invest Ophthalmol Vis Sci, 2023, 64(4):31] PubMed: 37099021
Sirtuin activation targets IDH-mutant tumors [ Neuro Oncol, 2021, 23(1):53-62] PubMed: 32710757

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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