1. Cell Cycle/DNA Damage
    Epigenetics
  2. Sirtuin

AK-1 

Cat. No.: HY-101465 Purity: >98.0%
Handling Instructions

AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor.

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

AK-1 Chemical Structure

AK-1 Chemical Structure

CAS No. : 330461-64-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
25 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

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  • References

Description

AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor.

IC50 & Target[2]

SIRT2

 

In Vitro

AK-1 achieves significant neuroprotection in Huntington’s disease flies at 10 μM, improving the number of rhabdomeres from 5.2 to 5.6[1]. AK-1 treatment induces proteasomal degradation of the Snail transcription factor through inactivation of the NF-κB/CSN2 pathway. Reduction in the level of Snail results in upregulation of p21, leading to G1 arrest, slow proliferation, and slow wound-healing activity. The regulation of Snail-p21 axis by AK-1 also occurs in HT-29 colon cancer cells[2]. Under hypoxic conditions, AK-1 increases the ubiquitination of HIF-1α in a VHL-dependent manner, leading to the degradation of HIF-1α via a proteasomal pathway. Downregulation of HIF-1α expression reduces its transcriptional activity and, eventually, reduces the expression of BNIP3, one of HIF-1 target genes, in AK-1-treated cells[3].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4786 mL 12.3931 mL 24.7862 mL
5 mM 0.4957 mL 2.4786 mL 4.9572 mL
10 mM 0.2479 mL 1.2393 mL 2.4786 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[3]

HEK293 cells are co-transfected with 3 μg of pGL2-PGK1-HRE-Luc and 1 μg of pCMV-β-galactosidase plasmids. Twenty-four hours later, the cells are incubated under hypoxic conditions for 24 hr in the presence of 10 μM AK-1 and then lysed with luciferase cell lysis buffer. Luciferase and β-galactosidase activities are measured using luciferin and ο-nitrophenyl-β-d-galactopyranoside, respectively, as substrates. Transfection efficiency is normalized according to β-galactosidase activity[3].

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

References
Molecular Weight

403.45

Formula

C₁₉H₂₁N₃O₅S

CAS No.

330461-64-8

SMILES

O=C(NC1=CC=CC([N+]([O-])=O)=C1)C2=CC=CC(S(=O)(N3CCCCCC3)=O)=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AK-1
Cat. No.:
HY-101465
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AK-1

Cat. No.: HY-101465