1. Cell Cycle/DNA Damage Epigenetics
  2. Sirtuin
  3. SIRT3 activator 2

SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 improved the thermal stability of SIRT3 in SH-SY5Y cells, indicating that it can directly bind to SIRT3, has SIRT3 dependency in SH-SY5Y to clear α-Syn. SIRT3 activator 2 improves motor function in Parkinson mice, preventing Parkinson (DA) neuron loss in the substantia nigra in a dose-dependent manner.

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SIRT3 activator 2 Chemical Structure

SIRT3 activator 2 Chemical Structure

CAS No. : 3061491-60-6

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Description

SIRT3 activator 2 (compound 2a) is a SIRT3 activator. SIRT3 activator 2 improved the thermal stability of SIRT3 in SH-SY5Y cells, indicating that it can directly bind to SIRT3, has SIRT3 dependency in SH-SY5Y to clear α-Syn. SIRT3 activator 2 improves motor function in Parkinson mice, preventing Parkinson (DA) neuron loss in the substantia nigra in a dose-dependent manner[1].

IC50 & Target

SIRT3

 

In Vitro

SIRT3 activator 2 (10 μM, 100 μM) is a SIRT3 activator[1].
SIRT3 activator2 (10 μM; 24 h) enhances the thermal stability (CETSA) of SIRT3 in SH-SY5Y cells, indicating can bind directly to SIRT3 (WB) [1].
SIRT3 activator 2 (10 μM; 24 h) by SIRT3 dependency in SH-SY5Y cells, eliminats α-Syn (WB) to protects neurons.

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

Western Blot Analysis[1]

Cell Line: SH-SY5Y
Concentration: 10 μM
Incubation Time: 24 h
Result: Improved the thermal stability (CETSA) of SIRT3 in SH-SY5Y cells and could bind directly to SIRT3.

Apoptosis Analysis[1]

Cell Line: Ttransfected with SIRT3 siRNAs in SH-SY5Y cells.
Concentration: 10 μM
Incubation Time: 24 h
Result: Showed that the protective effect of SIRT3 activator 2 on MPP+ (600 μM) or 6-OHDA(100μM)-induced neuronal injury disappeared and the expression level of α-Syn did not change significantly after SIRT3 silences.
In Vivo

SIRT3 activator 2 (10, 20, 40 mg/kg; Intravenous injection (i.v.); Once daily; 24 days) improves overexpression of A53T α-synuclein-induced motor function in Parkinson mice[1].
SIRT3 activator 2 (10, 20, 40 mg/kg; Intracerebroventricular injection (ICV)) dose-dependently prevents overexpression of A53T α-synuclein-induced loss of substantia nigra DA neurons (immunohistochemistry) [1].

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

Animal Model: Parkinson mouse model injected with overexpression of A53T α-synuclein[1]
Dosage: 10, 20, 40 mg/kg
Administration: Intravenous injection (i.v.);Once daily; 24 days;The viruses (2.5 x 1012 genomic particles/ml) were infused to the right substantia nigra of mouse
Result: Showed that the movement function of mice was improved by increasing the walking distance, decreasing the descending time on the rod and increasing the descending time on the rotating rod.
Molecular Weight

492.50

Formula

C22H24N2O9S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(CC1(C(N2CCC3=O)=O)CC2=O)(C(N1S(C4=CC(C(OCCCO3)=O)=CC=C4)(=O)=O)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 4.93 mg/mL (10.01 mM; Need ultrasonic; 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 2.0305 mL 10.1523 mL 20.3046 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0305 mL 10.1523 mL 20.3046 mL 50.7614 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 mL 10.1523 mL
10 mM 0.2030 mL 1.0152 mL 2.0305 mL 5.0761 mL
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  • 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.

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Product Name:
SIRT3 activator 2
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HY-163987
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