SRT2183

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

SRT2183 Chemical Structure

SRT2183 Chemical Structure

CAS: 1001908-89-9

Selleck's SRT2183 has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.19%
99.19

SRT2183 Related Products

Signaling Pathway

Choose Selective Sirtuin Inhibitors

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
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 468.57 Formula

C27H24N4O2S

CAS No. 1001908-89-9 SDF Download SRT2183 SDF
Smiles C1CN(CC1O)CC2=CSC3=NC(=CN23)C4=CC=CC=C4NC(=O)C5=CC6=CC=CC=C6C=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (198.47 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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