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AK 7
- Soluble in DMSO
- MF: C19H21BrN2O3S
- MW: 437.35
Description
Potent, brain-permeable and selective inhibitor of SIRT2 (IC50 values >50 μM, 15.5 μM, and >50 μM for SIRT1, SIRT2, and SIRT3 respectively. Treatment with AK 7 showed a SIRT2-dependent nucleo-cytoplasmic trafficking in primary striatal neurons of the master regulator of cholesterol biosynthesis, SREBP-2, and resulted in protection of neurons in an in vitro model of Huntington's disease (HD).
AK 7 is slightly less potent in vitro than its analogue AK 1 (Axon 2269).
More Information
| Parent CAS No. | 420831-40-9 |
|---|---|
| Chemical Name | 3-(azepan-1-ylsulfonyl)-N-(3-bromophenyl)benzamide |
| SMILES | C(NC1=CC=CC(Br)=C1)(=O)C1=CC=CC(S(N2CCCCCC2)(=O)=O)=C1 |
| MFCD | MFCD03140195 |
| InChi | InChI=1S/C19H21BrN2O3S/c20-16-8-6-9-17(14-16)21-19(23)15-7-5-10-18(13-15)26(24,25)22-11-3-1-2-4-12-22/h5-10,13-14H,1-4,11-12H2,(H,21,23) |
| InChiKey | IYAYHZZWYNXHEQ-UHFFFAOYSA-N |
| CID | 1328033 |
| Short Description | SIRT2 inhibitor |
References
- T.F. Outeiro et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007, 317, 516-519.
- R. Luthi-Carter et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc. Natl. Acad. Sci. USA. 2010, 107, 7927-7932.
- D.M. Taylor et al. A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase. ACS Chem. Biol. 2011, 6, 540-546.
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