SIRT2 Inhibitor II (AK-1) |
カタログ番号GC30922
One-Click Copy Product Info
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SIRT2 Inhibitor II (AK-1) は、強力で特異的な細胞透過性の SIRT2 阻害剤であり、IC50 は 12.5 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 330461-64-8
Sample solution is provided at 25 µL, 10mM.
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AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor.
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].
[1]. 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. [2]. 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. [3]. 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.
Cell experiment: | 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]. |
References: [1]. 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. | |
| Cas No. | 330461-64-8 | SDF | |
| Canonical SMILES | O=C(NC1=CC=CC([N+]([O-])=O)=C1)C2=CC=CC(S(=O)(N3CCCCCC3)=O)=C2 | ||
| Formula | C19H21N3O5S | M.Wt | 403.45 |
| 溶解度 | DMSO : ≥ 50 mg/mL (123.93 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4786 mL | 12.3931 mL | 24.7862 mL |
| 5 mM | 495.7 μL | 2.4786 mL | 4.9572 mL |
| 10 mM | 247.9 μL | 1.2393 mL | 2.4786 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)