SRT2104 (GSK2245840)

Catalog No.S7792

SRT2104 (GSK2245840) Chemical Structure

Molecular Weight(MW): 516.64

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.

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Biological Activity

Description SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
Targets
SIRT1 [1]
In vitro

SRT2104 reduces p65/RelA acetylation levels in C2C12 cells.[1]

In vivo In male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard diet, and enhances motor coordination, bone mineral density, and insulin sensitivity and decreased inflammation. Short-term SRT2104 treatment preserves bone and muscle mass in an experimental model of atrophy.[1] In Male N171-82Q HD mice, SRT2104 (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival.[2]

Protocol

Kinase Assay:[3]
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SIRT1 fluorescence polarization assay and HTS:

In the SIRT1 FP assay, SIRT1 activity is monitored using a 20 amino acid peptide (Ac-Glu-Glu-Lys(biotin)-Gly-Gln-Ser-Thr-Ser-Ser-His-Ser-Lys(Ac)-Nle-Ser-Thr-Glu-Gly–Lys(MR121 or Tamra)-Glu-Glu-NH2 ) derived from the sequence of p53. The peptide is N-terminally linked to biotin and C-terminally modified with a fluorescent tag. The reaction for monitoring enzyme activity is a coupled enzyme assay where the first reaction is the deacetylation reaction catalyzed by SIRT1 and the second reaction is cleavage by trypsin at the newly exposed lysine residue. The reaction is stopped and streptavidin is added in order to accentuate the mass differences between substrate and product. The fluorescence polarization reaction conditions are as follows: 0.5 μM peptide substrate, 150 μM βNAD +, 0-10 nM SIRT1, 25 mM Tris-acetate pH 8, 137 mM Na-Ac, 2.7 mM K-Ac, 1 mM Mg-Ac, 0.05% Tween-20, 0.1% Pluronic F127, 10 mM CaCl 2 , 5 mM DTT, 0.025% BSA, and 0.15 mM nicotinamide. The reaction is incubated at 37°C and stopped by addition of nicotinamide, and trypsin is added to cleave the deacetylated substrate. This reaction is incubated at 37 ℃ in the presence of 1 μM streptavidin. Fluorescent polarization is determined at excitation (650 nm) and emission (680 nm) wavelengths.
Cell Research:[1]
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  • Cell lines: C2C12 cell line
  • Concentrations: 3 μM
  • Incubation Time: 24 h
  • Method: Cells are cultured in low glucose Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum and penicillin–streptomycin. Cells are treated with vehicle (0.1% DMSO) or 3 μM SRT2104 for 24 h and then harvested for protein and Western blotting.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Male N171-82Q HD mice
  • Formulation: With diet
  • Dosages: diet containing 0.5% SRT2104
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL warmed (30.96 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 516.64
Formula

C26H24N6O2S2

CAS No. 1093403-33-8
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01702493 Completed Psoriasis Sirtris, a GSK Company|GlaxoSmithKline October 2012 Phase 1
NCT01453491 Completed Colitis, Ulcerative Sirtris, a GSK Company|GlaxoSmithKline February 2012 Phase 1
NCT01039909 Withdrawn Healthy Volunteer|Atrophy, Muscular GlaxoSmithKline January 2011 Phase 1
NCT01154101 Completed Psoriasis Sirtris, a GSK Company|GlaxoSmithKline June 2010 Phase 2
NCT01031108 Completed Diabetes Mellitus, Type 2 Sirtris, a GSK Company|GlaxoSmithKline May 2010 Phase 1
NCT01018017 Completed Diabetes Mellitus, Type 2 GlaxoSmithKline March 2010 Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID