Art. -Nr.: HY-100578

AGK2

20 Cited Publications

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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.

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Reinheit: 99.43%
CAS. Nr.: 304896-28-4
Formel: C₂₃H₁₃Cl₂N₃O₂
Molecular Weight:434.27

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

AGK2 Chemical Structure

CAS. Nr.: 304896-28-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target^[1]

SIRT2

3.5 μM (IC₅₀)

SIRT1

30 μM (IC₅₀)

SIRT3

91 μM (IC₅₀)

Alle Sirtuin Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

In Vitro

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.

In Vivo

AGK2 significantly reduces mortality and decreases levels of cytokines 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) compare to vehicle control. AGK2 also suppresses the TNF-α and IL-6 production in the culturing splenocytes (TNF-α: 68.1±6.4 vs 23.9±2.8 pg/mL, p=0.0009; IL-6: 73.1±4.2 vs 49.6±3.0 pg/mL; p=0.0051)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 304896-28-4
Appearance Solid
Molecular Weight 434.27
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (20)

All Bio/Physico-chemical AssayIn Vivo Efficacy StudyHistological Imaging/StainingWB

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Journal Impact Factor

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

Electrochemical Oxidation of Sulfonamides with Boron-Doped Diamond and Pt Anodes. [Abstract]

2019 Dec 13;8(12):1421-1428. PMID: 31867150
Acta Pharm Sin B

A one-step specific assay for continuous detection of sirtuin 2 activity. [Abstract]

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

Enhancing intestinal epithelial microtubule stability could alleviate IBD symptoms. [Abstract]

2025 Jun 4;23(1):263. PMID: 40462136
Phytomedicine

Ginsenoside Rc maintains sleep rhythm homeostasis by alleviating oxidative stress. [Abstract]

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

SIRT2 alleviates pre-eclampsia via prompting mitochondrial biogenesis and function. [Abstract]

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

HK2 promotes angiogenesis through H3K18 lactylation in peripheral arterial disease. [Abstract]

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
SSRN

2025 Aug 8.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Protokoll

Cell Assay^[2]

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.

Animal Administration^[4]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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AGK2

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Antioxidant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AGK2

Alle Sirtuin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AGK2

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Antioxidant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AGK2

Alle Sirtuin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AGK2 Related Classifications

HY-100578 Related Classifications