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SRT 2104

Catalog No. T6679 CAS 1093403-33-8

Synonyms: SRT2104, sirtuin modulator, GSK2245840

SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SRT 2104, CAS 1093403-33-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 243.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 593.00
200 mg	In stock	$ 848.00
500 mg	In stock	$ 1,290.00
1 g	In stock	$ 1,730.00
1 mL * 10 mM (in DMSO)	In stock	$ 113.00

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Purity: 99.83%

Purity: 99.82%

Purity: 99.45%

Purity: 99.35%

Purity: 97.03%

Biological Description

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Storage & Solubility Information

Description	SRT 2104 (GSK2245840) is a selective and brain-permeable SIRT1 activator.
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]
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	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)

Synonyms	SRT2104, sirtuin modulator, GSK2245840
Molecular Weight	516.64
Formula	C26H24N6O2S2
CAS No.	1093403-33-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 13 mg/mL (25.2 mM)

References and Literature

1. Mercken EM, et al. Aging Cell. 2014, 13(5), 787-796. 2. Jiang M, et al. Ann Clin Trans Neurol. 2014, 1(12), 1047-1052. 3. Milne JC, et al. Nature. 2007, 450(7170), 712-716.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Glutamine Metabolism Compound Library Anti-Diabetic Compound Library Bioactive Compounds Library Max DNA Damage & Repair Compound Library Anti-Metabolism Disease Compound Library CNS-Penetrant Compound Library Clinical Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SRT 2104 1093403-33-8 Chromatin/Epigenetic DNA Damage/DNA Repair Sirtuin SRT2104 sirtuin modulator GSK-2245840 GSK2245840 SRT-2104 Inhibitor GSK 2245840 inhibit inhibitor

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