20S Proteasome activator 1

Name: 20S Proteasome activator 1
Brand: MedChemExpress
SKU: HY-150602
Rating: 4.5 (1 reviews)

Cat. No.: HY-150602 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

20S Proteasome activator 1 is a potent 20S proteasome activator with EC₂₀₀ values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases.

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

20S Proteasome activator 1 Chemical Structure

CAS No. : 2761578-18-9

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 125	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	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

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC₅₀: 0.3 μM (trypsin-like site), 0.7 μM (chymotrypsin-like site), 1.8 μM (caspase-like site)^[1]

In Vitro

20S Proteasome activator 1 (compound 19) (2.5-15 μM; 45 min) degrades 73% α-synuclein at 10 μM, and over 80% at 15 μM^[1].
20S Proteasome activator 1 (5-15 μM; 24 h) reduces 25% A53T mutant, and dose-dependently reduces enhancement of α-synuclein in Hek-293T cells (transiently transfected with an A53T mutant α-synuclein plasmid) at 5 μM; decreases 67% A53T α-synuclein at 15 μM^[1].

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

Molecular Weight

492.97

Formula

C₂₇H₁₉ClF₂N₂OS

CAS No.

2761578-18-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C1=CC=C(F)C=C1)C2=CC=C(F)C=C2)CCN3C4=C(C=CC=C4)SC5=CC=C(Cl)C=C35

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (202.85 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	2.0285 mL	10.1426 mL	20.2852 mL
5 mM	0.4057 mL	2.0285 mL	4.0570 mL
10 mM	0.2029 mL	1.0143 mL	2.0285 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

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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.07 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: 99.83%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (254 KB) HNMR (262 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. Staerz SD, et al. Design, Synthesis, and Biological Evaluation of Potent 20S Proteasome Activators for the Potential Treatment of α-Synucleinopathies. J Med Chem. 2022 May 12;65(9):6631-6642. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0285 mL	10.1426 mL	20.2852 mL	50.7130 mL
	5 mM	0.4057 mL	2.0285 mL	4.0570 mL	10.1426 mL
	10 mM	0.2029 mL	1.0143 mL	2.0285 mL	5.0713 mL
	15 mM	0.1352 mL	0.6762 mL	1.3523 mL	3.3809 mL
	20 mM	0.1014 mL	0.5071 mL	1.0143 mL	2.5357 mL
	25 mM	0.0811 mL	0.4057 mL	0.8114 mL	2.0285 mL
	30 mM	0.0676 mL	0.3381 mL	0.6762 mL	1.6904 mL
	40 mM	0.0507 mL	0.2536 mL	0.5071 mL	1.2678 mL
	50 mM	0.0406 mL	0.2029 mL	0.4057 mL	1.0143 mL
	60 mM	0.0338 mL	0.1690 mL	0.3381 mL	0.8452 mL
	80 mM	0.0254 mL	0.1268 mL	0.2536 mL	0.6339 mL
	100 mM	0.0203 mL	0.1014 mL	0.2029 mL	0.5071 mL