SRT2183

Catalog No.S8270 Batch:S827002

Technical Data

Formula	C₂₇H₂₄N₄O₂S
Molecular Weight	468.57	CAS No.	1001908-89-9
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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

Targets

SIRT1 ^[1]

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].

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines Bone-marrow derived macrophages(BMMs) Concentrations 1μM Incubation Time 72 h Method 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.

Cell Assay:^{^[4]}

Cell lines
Bone-marrow derived macrophages(BMMs)
Concentrations
1μM
Incubation Time
72 h
Method
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.

References

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

+ Expand

Selleck's SRT2183 has been cited by 6 publications

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
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

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SHIPPING AND STORAGE
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