AGK2

Name: AGK2
Brand: MedChemExpress
SKU: HY-100578
Rating: 5.0 (11 reviews)

Cat. No.: HY-100578 Purity: 99.62%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

AGK2 Chemical Structure

CAS No. : 304896-28-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 93	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 93	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 610	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE AGK2

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sirtuin Isoform Specific Products:

View All Isoforms

Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

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.

Molecular Weight

434.27

Formula

C₂₃H₁₃Cl₂N₃O₂

CAS No.

304896-28-4

Appearance

Solid

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.62%

Select Batch:

Data Sheet (281 KB) SDS (394 KB)

COA (251 KB) LCMS (133 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]

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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AGK2304896-28-4AGK 2AGK-2SirtuinApoptosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

AGK2

Customer Review

AGK2 Related Antibodies

11 Publications Citing Use of MCE AGK2

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sirtuin Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AGK2 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AGK2 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report