| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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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].
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| 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].
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| References |
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| Additional Infomation |
2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-(5-quinolinyl)-2-propenamide is a member of quinolines.
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| Molecular Formula |
C23H13CL2N3O2
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| Molecular Weight |
434.27
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| Exact Mass |
433.038
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| CAS # |
304896-28-4
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| Related CAS # |
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| PubChem CID |
2130404
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
675.1±55.0 °C at 760 mmHg
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| Flash Point |
362.1±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.718
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| LogP |
5.39
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
706
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=CC=N2)C(=C1)NC(=O)/C(=C/C3=CC=C(O3)C4=C(C=CC(=C4)Cl)Cl)/C#N
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| InChi Key |
SVENPFFEMUOOGK-SDNWHVSQSA-N
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| 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+
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| Chemical Name |
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
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| Synonyms |
AGK-2; AGK-2; AGK-2.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 8% DMSO+30% PEG 300+ddH2O:~1.5 mg/mL |
| 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.
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