Revision 1

#36804Store at RT

5 mg

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

3 Trask LaneDanversMassachusetts01923USA
For Research Use Only. Not for Use in Diagnostic Procedures.

Background

The brain-permeable small-molecule AK-7 inhibits the NAD-dependent deacetylase sirtuin 2 (SirT2) which is involved in cytoskeletal regulation and progression through mitosis. The inhibitor AK-7 specifically binds and inhibits SirT2 (IC50 = 15.5 mM) and has no apparent effect on SirT1 or SirT3. AK-7 reduced total cholesterol in primary striatal neurons and reduced cholesterol in cultured naïve neuronal cells and brain slices from wild-type mice (1). Treatment with AK-7 improved motor function, extended survival, and reduced brain atrophy in a pair of genetic mouse models of Huntington’s disease (2). In a study of aging in a rat model of Parkinson's disease, AK-7 inhibition revealed a potential role for SirT2 in Parkinson's neurodegeneration, and suggested that AK-7 may have a beneficial neuroprotective effect (3). Similar results were seen in a mouse model of Parkinson's disease, but AK-7 was not able to counteract neurodegenerative processes associated with amyotrophic lateral sclerosis (ALS) or cerebral ischemia (4).

  1. Taylor, D.M. et al. (2011) ACS Chem Biol 6, 540-6.
  2. Chopra, V. et al. (2012) Cell Rep 2, 1492-7.
  3. Wang, X. et al. (2015) Drug Des Devel Ther 9, 2553-63.
  4. Chen, X. et al. (2015) PLoS One 10, e0116919.

Molecular Formula

C19H21BrN2O3S

Molecular Weight

437.4 g/mol

Purity

>98%

CAS

420831-40-9

Solubility

Soluble in DMSO at 50 mg/mL or ethanol at 8 mg/mL.

Storage

Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Directions for Use

AK-7 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.14 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Background References

    Cross-Reactivity Key

    H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

    Trademarks and Patents

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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