Identification | Back Directory | [Name]
SIRT2 Inhibitor II, AK-1 | [CAS]
330461-64-8 | [Synonyms]
CS-923 AK 1, >=98% AK-1;AK1;AK 1 AK-1 >=98% (HPLC) SIRT2 Inhibitor II, AK-1 Benzamide, 3-[(hexahydro-1H-azepin-1-yl)sulfonyl]-N-(3-nitrophenyl)- 3-(azepane-1-sulfonyl)-N-(3-nitro-phenyl)-benzamide SIRT2 Inhibitor II, AK-1 | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C19H21N3O5S | [MOL File]
330461-64-8.mol | [Molecular Weight]
403.45 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml; Ethanol: 0.3 mg/ml | [form ]
A crystalline solid | [color ]
White to off-white |
Hazard Information | Back Directory | [Description]
AK-1 is a SIRT2 Inhibitor II that prevents hippocampal neurodegeneration in Alzheimer's disease models and induces cell cycle arrest in colon carcinoma cells. | [Uses]
AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50 of 12.5 μM. | [IC 50]
SIRT2: 12.5 μM (IC50) | [storage]
Store at -20°C | [References]
[1] Ruth Luthi-Carter, et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc Natl Acad Sci U S A. 2010 Apr 27;107(17):7927-32. DOI:10.1073/pnas.1002924107 [2] Lee SD, et al. AK-1, a SIRT2 inhibitor, destabilizes HIF-1α and diminishes its transcriptional activity during hypoxia. Cancer Lett. 2016 Apr 1;373(1):138-45. DOI:10.1016/j.canlet.2016.01.031 [3] Luthi-Carter R, et al. SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis. Proc Natl Acad Sci U S A. 2010 Apr 27;107(17):7927-32. [4] David M. Taylor, et al. A Brain-Permeable Small Molecule Reduces Neuronal Cholesterol by Inhibiting Activity of Sirtuin 2 Deacetylase. ACS Chem Biol. 2011 Jun 17;6(6):540-6. DOI:10.1021/cb100376q [5] Cheon MG, et al. AK-1, a specific SIRT2 inhibitor, induces cell cycle arrest by downregulating Snail in HCT116 human colon carcinoma cells. Cancer Lett. 2015 Jan 28;356(2 Pt B):637-45. DOI:10.1016/j.canlet.2014.10.012 |
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