SRT2183

製品コードS8270 バッチS827002

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

C27H24N4O2S
分子量 468.57 CAS No. 1001908-89-9
Solubility (25°C)* 体外 DMSO 93 mg/mL (198.47 mM)
Ethanol 8 mg/mL (17.07 mM)
Water 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 SRT2183は、現在Sirtris Pharmaceuticals社によって開発されている、サーチュインサブタイプSIRT1の低分子活性化因子です。
in vitro SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. This compound treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes. SRT1720, this chemical, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. It has little or no effect on SIRT1 deacetylating activity with native full-length substrates. This compound activates AMPK, increases Sirt1 expression and decreases RelA/p65 lysine310 acetylation, critical for NF-κB activation, and an established Sirt1 target and inhibits RANKL-induced osteoclast generation and resorptive capacity in bone marrow macrophages.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Bone-marrow derived macrophages(BMMs)
濃度 1μM
反応時間 72 h
実験の流れ BMMs are harvested, plated and 24-hrs later non-adherent cells were re-plated at a density of 20,000 cells/well in α-MEM/15%FBS/5% M-CSF. For determining cell proliferation, cells are treated with SRT2183 or a vehicle for 72 hours post plating and BrdU reagent is added 48 hrs post this compound or vehicle administration according to the manufacturer's instructions to determine cell proliferation 3 days post plating.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18046409/
  • http://www.bloodjournal.org/content/114/22/3083?sso-checked=true
  • https://pubmed.ncbi.nlm.nih.gov/20061378/
  • https://pubmed.ncbi.nlm.nih.gov/20061378/

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：

Neutrophils shape the therapeutic efficacy of sirtuin 1 activity modulators in murine influenza virus infection [ Biochim Biophys Acta Mol Basis Dis, 2025, 1871(7):167915] PubMed: 40419167
SIRT1 and HSP90α feed-forward circuit safeguards chromosome segregation integrity in diffuse large B cell lymphomas [ Cell Death Dis, 2023, 14(10):667] PubMed: 37816710
SRT2183 and SRT1720, but not Resveratrol, Inhibit Osteoclast Formation and Resorption in the Presence or Absence of Sirt1 [ J Bone Res, 2023, 11(4)1000235] PubMed: 37711761
Sirtuin activation targets IDH-mutant tumors [ Neuro Oncol, 2021, 23(1):53-62] PubMed: 32710757
Lactate promotes macrophage HMGB1 lactylation, acetylation, and exosomal release in polymicrobial sepsis [ Cell Death Differ, 2021, 10.1038/s41418-021-00841-9] PubMed: 34363018
Sirt1 attenuates diabetic keratopathy by regulating the endoplasmic reticulum stress pathway [ Life Sci, 2020, S0024-3205(20)31542-3] PubMed: 33220291

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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