Home DNA Damage/DNA Repair Sirtuin activator SRT2104 (GSK2245840) For research use only.

SRT2104 (GSK2245840)

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

SRT2104 (GSK2245840) Chemical Structure

SRT2104 (GSK2245840) Chemical Structure

CAS No. 1093403-33-8

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SRT2104 (GSK2245840) Related Products

Signaling Pathway

Sirtuin Signaling Pathways

Sirtuin Signaling Pathway

Biological Activity

Description SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
Targets
SIRT1 [1]
In vitro
In vitro SRT2104 reduces p65/RelA acetylation levels in C2C12 cells.[1]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Male N171-82Q HD mice
Dosages diet containing 0.5% SRT2104
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01453491 Completed
Colitis Ulcerative
Sirtris a GSK Company|GlaxoSmithKline
 February 13 2012 Phase 1
NCT01039909 Withdrawn
Healthy Volunteer|Atrophy Muscular
GlaxoSmithKline
 January 2011 Phase 1
NCT01154101 Completed
Psoriasis
Sirtris a GSK Company|GlaxoSmithKline
 June 7 2010 Phase 2
NCT01031108 Completed
Diabetes Mellitus Type 2
Sirtris a GSK Company|GlaxoSmithKline
 May 28 2010 Phase 1
NCT01018017 Completed
Diabetes Mellitus Type 2
GlaxoSmithKline
 March 3 2010 Phase 2

Chemical Information & Solubility

Molecular Weight 516.64 Formula

C26H24N6O2S2
CAS No. 1093403-33-8 SDF Download SRT2104 (GSK2245840) SDF
Smiles CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 4 mg/mL ( (7.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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