SIRT2 Inhibitor II, AK-1 Chemical Properties

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

SIRT2 Inhibitor II, AK-1 Usage And Synthesis

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)

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