1. Cell Cycle/DNA Damage
    Epigenetics
  2. Sirtuin
  3. AK-7

AK-7 

Cat. No.: HY-16691 Purity: 99.91%
Handling Instructions

AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.

For research use only. We do not sell to patients.

AK-7 Chemical Structure

AK-7 Chemical Structure

CAS No. : 420831-40-9

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10 mM * 1 mL in DMSO USD 145 In-stock
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10 mg USD 132 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.

IC50 & Target[1]

SIRT2

15.5 μM (IC50)

In Vitro

AK-7 (10 μM) reduces cholesterol levels in naive N2a neuroblastoma cells and hippocampal slice cultures from wild-type mice. AK-7 (1 μM) shows neuroprotective effect of AK-7 in striatal Huntington’s disease (HD) neurons[1]. AK-7 (12.5 μM) decreases ratio of DA neurons in primary midbrain cultures[3].

In Vivo

AK-7 (15 mg/kg/dose, i.p.) is brain-permeable in wild-type and HD mice[1]. AK-7 (10, 20 mg/kg, i.p.) improves the behavior and neuropathological phenotype and extends survival of R6/2 HD mice. AK-7 (20 mg/kg) ameliorates HD neuropathology in R6/2 mice. AK-7 also reduces the polyglutamine aggregation in R6/2 brain. In addition, AK-7 treated 140CAG mice show motor performance changes that parallel untreated wild-type mice, with the 20 mg/kg dose being most effective and significantly different from untreated 140CAG mice[2].

Molecular Weight

437.35

Formula

C₁₉H₂₁BrN₂O₃S

CAS No.

420831-40-9

SMILES

O=S(N1CCCCCC1)(C2=CC(C(NC3=CC(Br)=CC=C3)=O)=CC=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (114.32 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2865 mL 11.4325 mL 22.8650 mL
5 mM 0.4573 mL 2.2865 mL 4.5730 mL
10 mM 0.2286 mL 1.1432 mL 2.2865 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.72 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.72 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Neuronal nuclear antigen (NeuN)-positive neurons and some astroglia are derived from mechanically dissociated ganglionic eminences of E16 rat embryos. The HD model is based on the expression of mutant huntingtin. Treatments of cultures with AK-7 are at 10 μM for 24 h unless stated otherwise. DMSO is included at the same concentrations as a control. Lower dose, chronic treatments with AK-7 are introduced to neurons at DIV4 and continued weekly coinciding with normal medium change[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

AK-7, solubilized at 1.5 mg/mL in 25% Cremophor EL (BASF)/ 10% DMSO in water, is administered by intraperitoneal injection to 11 week old mice at 15 mg/kg/dose, and compound levels in serum and brain are measured following sacrifice. Blood is collected and centrifuged at 7,000 rpm for 7 min, and then serum is aspirated and immediately frozen in liquid nitrogen. Brains are immediately frozen in liquid nitrogen and stored at −80°C. Brains are weighed and then homogenized in four volumes of 10% Cremophor RH40 in water using a Polytron homogenizer, and 2% v/v phosphoric acid is added to the homogenate, vortexed, and centrifuged at 10,000 g at 25°C for 1 h. The supernatant is aspirated, and solid phase extraction is performed immediately. Serum samples are vortexed into 2% v/v phosphoric acid and centrifuged at 2500 rpm for 10 min[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.91%

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