| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
AGK2 is a novel, potent, and selective inhibitor of SIRT2 (sirtuin 2, histone deacetylase) with potential anti-inflammatory activity. As a cell-permeable epigenetic modifier, AGK2 inhibits SIRT2 with an IC50 value of 3.5 μM and showed little effects on SIRT1 and 3 at concentrations of over 40 μM. AGK 2 increased the level of acetylated tubulin heterodimers in bovine brain. In primary rat astrocytes, AGK-2 (35 μM) significantly inhibited astrocyte viability and proliferation and also inhibited astrocyte activation induced by beta amyloid 1-42 (Aβ 1-42).
| ln Vitro |
Cell growth is strongly inhibited by AGK2 in a dose-dependent manner. Additionally, in a dose-dependent way, AGK2 strongly suppresses cell growth without causing cytotoxicity at low concentrations. After being treated with AGK2 (5 μM) for 12 days, the cells' ability to form colonies in soft agar decreases significantly, reaching 46% of the control cells. A dose-dependent reduction in CDK4 or CDK6 and cyclin D1 levels is observed following AGK2 treatment, according to Western blot analysis. Furthermore, p53 protein expression is inhibited by AGK2[2]. PAR signals are significantly increased when 10 μM AGK2 is applied to microglial BV2 cells. When microglial BV2 cells are treated with 10 μM AGK2, there is a notable reduction in intracellular ATP and a notable elevation in both late-stage apoptosis and necrosis of the cells [3].
|
||
|---|---|---|---|
| ln Vivo |
In comparison to vehicle control, AGK2 significantly lowers mortality and cytokine levels in blood (TNF-α: 298.3±24.6 vs 26.8±2.8 pg/mL, p=0.0034; IL-6: 633.4±82.8 vs 232.6±133.0 pg/mL, p=0.0344) and peritoneal fluid (IL-6: 704.8±67.7 vs 391.4±98.5 pg/mL, p=0.033). Additionally, AGK2 inhibits the generation of IL-6 and TNF-α in cultured splenocytes (IL-6: 73.1±4.2 vs 49.6±3.0 pg/mL; p=0.0051; TNF-α: 68.1 ±6.4 vs 23.9±2.8 pg/mL, p=0.0009)[4].
|
||
| Animal Protocol |
|
||
| References |
[1]. Tatum PR, et al. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1871-4.
[2]. Kim HW, et al. Sirtuin inhibitors, EX527 and AGK2, suppress cell migration by inhibiting HSF1 protein stability. Oncol Rep. 2016 Jan;35(1):235-42. [3]. Li Y, et al. Poly(ADP-ribose) polymerase mediates both cell death and ATP decreases in SIRT2 inhibitor AGK2-treated microglial BV2 cells. Neurosci Lett. 2013 Jun 7;544:36-40. [4]. Zhao T, et al. Selective Inhibition of SIRT2 Improves Outcomes in a Lethal Septic Model. Curr Mol Med. 2015;15(7):634-41 |
| Molecular Formula |
C23H13CL2N3O2
|
|
|---|---|---|
| Molecular Weight |
434.27
|
|
| CAS # |
304896-28-4
|
|
| Related CAS # |
|
|
| SMILES |
O=C(NC1=C2C=CC=NC2=CC=C1)/C(C#N)=C/C3=CC=C(C4=CC(Cl)=CC=C4Cl)O3
|
|
| InChi Key |
SVENPFFEMUOOGK-SDNWHVSQSA-N
|
|
| InChi Code |
InChI=1S/C23H13Cl2N3O2/c24-15-6-8-19(25)18(12-15)22-9-7-16(30-22)11-14(13-26)23(29)28-21-5-1-4-20-17(21)3-2-10-27-20/h1-12H,(H,28,29)/b14-11+
|
|
| Chemical Name |
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
|
|
| Synonyms |
AGK-2; AGK-2; AGK-2.
|
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3027 mL | 11.5136 mL | 23.0271 mL | |
| 5 mM | 0.4605 mL | 2.3027 mL | 4.6054 mL | |
| 10 mM | 0.2303 mL | 1.1514 mL | 2.3027 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
COA