| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
| ln Vitro |
On Drosophila with Huntington's disease, AK-1 at 10 μM had a strong neuroprotective effect, increasing the number of striated muscles from 5.2 to 5.6 [1]. With an IC50 of 12.5 μM, AK-1 is a powerful, selective, and cell-permeable inhibitor of SIRT2 [2]. By blocking the NF-κB/CSN2 pathway, AK-1 therapy causes the Snail transcription factor to be broken down by proteases. Decreased snail levels cause p21 to be overexpressed, which slows down wound healing, G1 arrest, and proliferation. In HT-29 colon cancer cells, AK-1 also regulates the Snail-p21 axis [3]. In hypoxic environments, AK-1 enhances HIF-1α's ubiquitination in a VHL-dependent manner, which triggers HIF-1α's destruction via the proteasomal route. Downregulating HIF-1α expression in AK-1-treated cells lowers its transcriptional activity, which in turn lowers the expression of BNIP3, one of the HIF-1 target genes [4].
|
|---|---|
| References |
[1]. Ruth Luthi-Carter, 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]. 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. [3]. 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. [4]. David M. Taylor, et al. A Brain-Permeable Small Molecule Reduces Neuronal Cholesterol by Inhibiting Activity of Sirtuin 2 Deacetylase. ACS Chem Biol. 2011 Jun 17;6(6):540-6. [5]. 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 |
| Molecular Formula |
C19H21N3O5S
|
|---|---|
| Molecular Weight |
403.4521
|
| CAS # |
330461-64-8
|
| SMILES |
S(C1=C([H])C([H])=C([H])C(C(N([H])C2C([H])=C([H])C([H])=C(C=2[H])[N+](=O)[O-])=O)=C1[H])(N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])(=O)=O
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~123.93 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
