AGK2
Based on 20 publication(s) in Google Scholar
AGK2 is a selective SIRT2 inhibitor with an IC50 of 3.5 μM. AGK2 inhibits SIRT1 and SIRT3 with IC50s of 30 and 91 μM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.43%
- CAS No.: 304896-28-4
- Formula: C23H13Cl2N3O2
- Molecular Weight:434.27
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
Histone Modification Research Compound Library
HY-L024
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Covalent Screening Library
HY-L036
-
Antioxidant Compound Library
HY-L037
-
Reprogramming Compound Library
HY-L039
-
Oxygen Sensing Compound Library
HY-L045
-
Glutamine Metabolism Compound Library
HY-L064
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Multi-Target Compound Library
HY-L176
-
Radioprotector Library
HY-L178
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
Epigenetics Compound Library Mini
HY-L005M
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) AGK2
More- Theranostics. 2021 Feb 25;11(9):4381-4402. [Abstract]
- Acta Pharm Sin B. 2019 Dec 13;8(12):1421-1428. [Abstract]
- Acta Pharm Sin B. 2019 Nov;9(6):1183-1192. [Abstract]
- MedComm (2020). 2025 Mar 18;6(4):e70142. [Abstract]
- Cell Commun Signal. 2025 Jun 4;23(1):263. [Abstract]
- Phytomedicine. 2025 Jun:141:156634. [Abstract]
- Phytother Res. 2024 Sep;38(9):4628-4649. [Abstract]
- Free Radic Biol Med. 2026 Mar 16:246:381-393. [Abstract]
- Cell Rep. 2024 Dec 13;43(12):115060. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jan 15:270:115877. [Abstract]
- Biochem Pharmacol. 2026 Jan;243(Pt 1):117519. [Abstract]
- Life Sci. 2025 Mar 19:123566. [Abstract]
- J Am Heart Assoc. 2022 Jul 5;11(13):e025266. [Abstract]
- Commun Biol. 2026 May 28. [Abstract]
- Int Immunopharmacol. 2022 Sep:110:109000. [Abstract]
- Int Immunopharmacol. 2021 Sep:98:107841. [Abstract]
- iScience. 2020 Aug 21;23(8):101431. [Abstract]
- Biochem Biophys Res Commun. 2021 Sep 16;578:77-83. [Abstract]
- SSRN. 2025 Aug 8.
- Biomed Pharmacother. 2024 Jul 6:177:117085. [Abstract]
Customer Validation & Images
-
In Vivo Efficacy Study
-
Histological Imaging/Staining
-
WB
-
WB
-
Bio/Physico-chemical Assay
Biological Activity
|
SIRT2 3.5 μM (IC50) |
SIRT1 30 μM (IC50) |
SIRT3 91 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Hs 683 | IC50 |
80.2 μM
Compound: 4; AGK2
|
Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay
Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay
|
[PMID: 28475330] |
| U-373MG ATCC | IC50 |
47.6 μM
Compound: 4; AGK2
|
Antiproliferative activity against human U373 cells after 72 hrs by MTT assay
Antiproliferative activity against human U373 cells after 72 hrs by MTT assay
|
[PMID: 28475330] |
AGK2 significantly inhibits cell proliferation in a dose-dependent manner. AGK2 also significantly inhibits cell growth in a dose-dependent manner without inducing cytotoxicity at low doses. Twelve days after AGK2 (5 μM) treatment, cells show a significantly reducing colony forming ability in soft agar to 46% of the control cells. Western blot analysis shows that the levels of CDK4 or CDK6 and cyclin D1 are decreased after AGK2 treatment in a dose-dependent manner. In addition, AGK2 inhibits the expression of p53 protein[2]. Treatment of microglial BV2 cells with 10 μM AGK2 leads to a significant increase in PAR signals. Treatment of microglial BV2 cells with 10 μM AGK2 also leads to a significant decrease in the intracellular ATP and significant increases in both late-stage apoptosis and necrosis of the cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 304896-28-4
-
Appearance Solid
-
Molecular Weight 434.27
-
Formula C23H13Cl2N3O2
-
Color Light yellow to yellow
-
SMILES
O=C(NC1=C2C=CC=NC2=CC=C1)/C(C#N)=C/C3=CC=C(C4=CC(Cl)=CC=C4Cl)O3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (20)
-
Journal Impact Factor
-
Most Recent
-
Theranostics
NAD+-boosting therapy alleviates nonalcoholic fatty liver disease via stimulating a novel exerkine Fndc5/irisin. [Abstract]2021 Feb 25;11(9):4381-4402. PMID: 33754067
AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402. [Abstract]
AGK2 (1 mg/kg/day) were injected intraperitoneally. Liver SIRT2 activity, liver NAD+ level, plasma NAD+ level, Serum ALT activity and serum irisin level were determined in five groups of mice. NAFLD model was induced by MCD diet for 4 weeks.
AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402. [Abstract]
AGK2 (1 mg/kg/day) were injected intraperitoneally. Representative images and quantitative analysis of lipid accumulation, NAFLD activity score, macrophage infiltration and liver fibrosis according to Oil Red O staining, H & E staining, F4/80 immunohistochemistry staining and Masson trichrome staining respectively.
AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402. [Abstract]
AGK2 (1 mg/kg/day) were injected intraperitoneally. Fndc5 protein expression in mice under normal or NAFLD status.
AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402. [Abstract]
AGK2 (1 mg/kg/day) were injected intraperitoneally. The liver tissues were lysed and then immunoprecipitated by anti-Fndc5 antibody followed by immunoblotting with anti-Acetylated-lysine (anti-Ac) or anti-Ubiquitin to monitor the acetylation or ubiquitination of endogenous Fndc5 in mice treated with NR or NR plus AGK2. AGK2 treatment significantly abolished the decreased acetylation and ubiquitination of Fndc5 by NR.
-
Acta Pharm Sin B
2019 Dec 13;8(12):1421-1428. PMID: 31867150 -
Acta Pharm Sin B
2019 Nov;9(6):1183-1192. PMID: 31867164
AGK2 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2019 Nov;9(6):1183-1192. [Abstract]
AGK2 at gradient concentrations (0, 0.2, 1, 6, 30, 100, and 500 μmol/L) in assay buffer at 37 °C for 30 min. Dose–response curves and IC50 value for AGK2 and SirReal2 examined by ne-D9-based assay and ne-K4a-based assay.
-
MedComm (2020)
Swimming Exercise Pretreatment Attenuates Postoperative Delirium-Like Behavior in Type 2 Diabetic Rats by Enhancing Mitochondrial Biogenesis Through Activation of SIRT2 Deacetylation. [Abstract]2025 Mar 18;6(4):e70142. PMID: 40104261 -
Cell Commun Signal
2025 Jun 4;23(1):263. PMID: 40462136 -
Phytomedicine
2025 Jun:141:156634. PMID: 40203472 -
Phytother Res
Fisetin disrupts mitochondrial homeostasis via superoxide dismutase 2 acetylation in pancreatic adenocarcinoma. [Abstract]2024 Sep;38(9):4628-4649. PMID: 39091056 -
Free Radic Biol Med
Transplantation of Mitochondria isolated from iPSC-MSCs mitigates doxorubicin-induced cardiomyopathy by inhibiting cardiomyocyte senescence. [Abstract]2026 Mar 16:246:381-393. PMID: 41581580 -
Cell Rep
Desuccinylation of TBK1 by SIRT5 regulates inflammatory response of macrophages in sepsis. [Abstract]2024 Dec 13;43(12):115060. PMID: 39673708 -
Ecotoxicol Environ Saf
Sodium benzoate induces pancreatic inflammation and β cell apoptosis partially via benzoylation. [Abstract]2024 Jan 15:270:115877. PMID: 38150747 -
Biochem Pharmacol
Wedelolide A induces ferroptosis and apoptosis in gastric cancer via keap1/Nrf2 modulation and ROS generation. [Abstract]2026 Jan;243(Pt 1):117519. PMID: 41192684 -
Life Sci
2025 Mar 19:123566. PMID: 40118268 -
J Am Heart Assoc
Colchicine Ameliorates Dilated Cardiomyopathy Via SIRT2-Mediated Suppression of NLRP3 Inflammasome Activation. [Abstract]2022 Jul 5;11(13):e025266. PMID: 35766262 -
Commun Biol
2026 May 28. PMID: 42209711 -
Int Immunopharmacol
JMJD3/H3K27me3 epigenetic modification regulates Th17/Treg cell differentiation in ulcerative colitis. [Abstract]2022 Sep:110:109000. PMID: 35777266 -
Int Immunopharmacol
Ginsenoside Rg3 attenuates angiotensin II-induced myocardial hypertrophy through repressing NLRP3 inflammasome and oxidative stress via modulating SIRT1/NF-κB pathway. [Abstract]2021 Sep:98:107841. PMID: 34153662 -
iScience
BxPC-3-Derived Small Extracellular Vesicles Induce FOXP3+ Treg through ATM-AMPK-Sirtuins-Mediated FOXOs Nuclear Translocations. [Abstract]2020 Aug 21;23(8):101431. PMID: 32798974 -
Biochem Biophys Res Commun
Upregulation of α enolase (ENO1) crotonylation in colorectal cancer and its promoting effect on cancer cell metastasis. [Abstract]2021 Sep 16;578:77-83. PMID: 34547627 -
-
Biomed Pharmacother
1,8-cineole ameliorates experimental diabetic angiopathy by inhibiting NLRP3 inflammasome-mediated pyroptosis in HUVECs via SIRT2. [Abstract]2024 Jul 6:177:117085. PMID: 38972150
Solvent & Solubility
DMSO : 10 mg/mL (23.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cells are exposed to different concentrations of AGK2 in 1 mL of 0.3% basal medium agar containing 10% FBS. The cultures are maintained at 37°C in a 5% CO2 incubator for 10-15 days, and the cell colonies are scored using an inverted microscope[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice are intraperitoneally given either AGK2 (82 mg/kg) in dimethyl sulfoxide (DMSO) or DMSO alone, and 2 h later subjects to CLP. Survival is monitored for 240 hours. AGK2-treating mice are grouped into (i) DMSO vehicle, and (ii) AGK2, with sham mice (operating but without any treatment) serving as controls. Peritoneal fluid and peripheral blood are examined at 24 and 48 hours for cytokine production[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Zhao T, et al. Selective Inhibition of SIRT2 Improves Outcomes in a Lethal Septic Model. Curr Mol Med. 2015;15(7):634-41. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3027 mL | 11.5136 mL | 23.0271 mL | 57.5679 mL |
| 5 mM | 0.4605 mL | 2.3027 mL | 4.6054 mL | 11.5136 mL | |
| 10 mM | 0.2303 mL | 1.1514 mL | 2.3027 mL | 5.7568 mL | |
| 15 mM | 0.1535 mL | 0.7676 mL | 1.5351 mL | 3.8379 mL | |
| 20 mM | 0.1151 mL | 0.5757 mL | 1.1514 mL | 2.8784 mL |
AGK2 Related Classifications
HY-100578 Related Classifications
Powered by Bioz