PROTAC Sirt2 Degrader-1

Name: PROTAC Sirt2 Degrader-1
Brand: MedChemExpress
SKU: HY-103636
Rating: 4.5 (1 reviews)

Cat. No.: HY-103636 Purity: 98.71%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC₅₀ of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC₅₀s>100 μM).

For research use only. We do not sell to patients.

PROTAC Sirt2 Degrader-1 Chemical Structure

CAS No. : 2098487-75-1

Size	Price	Stock	Quantity
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1485	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2380	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PROTAC Sirt2 Degrader-1

•Structure. 2024 Sep 28:S0969-2126(24)00385-X. [Abstract]

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sirtuin Isoform Specific Products:

View All Isoforms

Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

SIRT2

0.25 μM (IC₅₀)

In Vitro

PROTAC Sirt2 Degrader-1 (Compound 12; 10 μM, 1-6 hours) induces Sirt2 degradation in HeLa cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	HeLa cells
Concentration:	10 µM
Incubation Time:	1-6 hours
Result:	Caused Sirt2 degradation, but showed no effect on Sirt1 levels.

Molecular Weight

852.94

Formula

C₄₀H₄₀N₁₀O₈S₂

CAS No.

2098487-75-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C(CCC1=O)C(N1)=O)C2=O)C(C2=CC=C3)=C3OCC(NCCCCN4C=C(COC5=CC(CC6=CN=C(NC(CSC7=NC(C)=CC(C)=N7)=O)S6)=CC=C5)N=N4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (117.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1724 mL	5.8621 mL	11.7242 mL
5 mM	0.2345 mL	1.1724 mL	2.3448 mL
10 mM	0.1172 mL	0.5862 mL	1.1724 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 2.5 mg/mL (2.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 98.71%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (244 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.1724 mL	5.8621 mL	11.7242 mL	29.3104 mL
	5 mM	0.2345 mL	1.1724 mL	2.3448 mL	5.8621 mL
	10 mM	0.1172 mL	0.5862 mL	1.1724 mL	2.9310 mL
	15 mM	0.0782 mL	0.3908 mL	0.7816 mL	1.9540 mL
	20 mM	0.0586 mL	0.2931 mL	0.5862 mL	1.4655 mL
	25 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL
	30 mM	0.0391 mL	0.1954 mL	0.3908 mL	0.9770 mL
	40 mM	0.0293 mL	0.1466 mL	0.2931 mL	0.7328 mL
	50 mM	0.0234 mL	0.1172 mL	0.2345 mL	0.5862 mL
	60 mM	0.0195 mL	0.0977 mL	0.1954 mL	0.4885 mL
	80 mM	0.0147 mL	0.0733 mL	0.1466 mL	0.3664 mL
	100 mM	0.0117 mL	0.0586 mL	0.1172 mL	0.2931 mL