SRT2183

製品コードS8270 バッチS827002

化学情報

	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
* <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 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.
in vitro	SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. SRT2183 treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes^[2]. SRT1720, SRT2183, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. SRT2183 has little or no effect on SIRT1 deacetylating activity with native full-length substrates^[3]. SRT2183 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^[4].

製品説明

SRT2183 is a small-molecule activator of the sirtuin subtype SIRT1, currently being developed by Sirtris Pharmaceuticals.

in vitro

SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. SRT2183 treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes^[2]. SRT1720, SRT2183, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. SRT2183 has little or no effect on SIRT1 deacetylating activity with native full-length substrates^[3]. SRT2183 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^[4].

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 SRT2183 or vehicle administration according to the manufacturer's instructions to determine cell proliferation 3 days post plating.

参考

[4] Pacholec M, et al. J Biol Chem. 2010, 285(11):8340-51.

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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：

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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