AK-7 is a cell- and brain-permeable, selective sirtuin SIRT2 inhibitor (IC50 ~15.5 μM). AK-7 displays no effect on SIRT1 or SIRT3. It diminishes neuronal cell death induced by mutant huntingtin fragment. It also down-regulates cholesterol biosynthetic gene expression and reduces total cholesterol levels in neurons in vivo. In two genetic mouse models of Huntington’s disease, AK-7 treatment resulted in improved motor function, extended survival, and reduced brain atrophy. AK-7 is a good chemical probe to study SIRT2’s roles in metabolic diseases, cancer, age-related disorders, and neurodegenerative diseases.
CAS Number: 420831-40-9
Molecular Weight: 437.35
Chemical Name: N-hydroxycyclopent-1-enecarboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
AK-7 was used at 10-25 µM in vitro and in cellular assays.
AK-7 was administered by intraperitoneal injection to mice at 15-30 mg/kg/dose twice daily (formulation: 1.5 mg/mL in 25% Cremophor/10% DMSO in water).
- Taylor DM, et al. A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase. (2011) ACS Chem Biol. 6(6):540-6.
- Chopra V, et al. The sirtuin 2 inhibitor AK-7 is neuroprotective in Huntington's disease mouse models. (2012) Cell Rep. 2(6):1492-7.
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