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AK 1
- Soluble in DMSO
- MF: C19H21N3O5S
- MW: 403.45
Description
Potent inhibitor of SIRT with good selectivity for SIRT2 over SIRT1 and SIRT3 (IC50 values >50 μM, 12.5 μM, and >50 μM for SIRT1, SIRT2, and SIRT3 respectively. Short-term treatment with AK 1 produced large statistically significant changes in RNA expression in untransduced, Htt171-18Q- and Htt171-82Q-expressing neurons and confirm the hypothesis that AK 1-mediated neuroprotection is correlated with the negative regulation of sterol biosynthesis.
AK 1 is among the first brain-permeable SIRT2 inhibitors that mediate neuroprotective reduction of cholesterol biosynthesis in an in vitro Huntington’s disease model. More potent in vitro than its analogue AK 7 (Axon 2270).
More Information
| Parent CAS No. | 330461-64-8 |
|---|---|
| Chemical Name | 3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide |
| SMILES | C1(S(N2CCCCCC2)(=O)=O)C=C(C(=O)NC2C=CC=C([N+]([O-])=O)C=2)C=CC=1 |
| MFCD | MFCD01122550 |
| InChi | InChI=1S/C19H21N3O5S/c23-19(20-16-8-6-9-17(14-16)22(24)25)15-7-5-10-18(13-15)28(26,27)21-11-3-1-2-4-12-21/h5-10,13-14H,1-4,11-12H2,(H,20,23) |
| InChiKey | HAYBKCHPEBZNGW-UHFFFAOYSA-N |
| CID | 1341463 |
| 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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