SRT2183

Catalog No.S8270 Batch:S827001

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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 3 mg/mL (6.4 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.)

Preparing Stock Solutions

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.

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
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.