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WRR139

Catalog No. T80771 Copy Product Info
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WRR139 is a peptide vinyl sulfone derivative that acts as a potent inhibitor of cytosolic N-glycanase 1 (NGLY1) and the transcription factor Nrf1. NGLY1-mediated deglycosylation is essential for the maturation and activation of Nrf1. By inhibiting NGLY1, WRR139 impairs Nrf1 processing, localization, and activation, thereby suppressing the compensatory expression of proteasome genes. WRR139 significantly potentiates the cytotoxicity of Carfilzomib against cancer cells, serving as a valuable tool for studying proteostasis and overcoming resistance to proteasome inhibitors.

WRR139

Copy Product Info
🥰Excellent
Catalog No. T80771

WRR139 is a peptide vinyl sulfone derivative that acts as a potent inhibitor of cytosolic N-glycanase 1 (NGLY1) and the transcription factor Nrf1. NGLY1-mediated deglycosylation is essential for the maturation and activation of Nrf1. By inhibiting NGLY1, WRR139 impairs Nrf1 processing, localization, and activation, thereby suppressing the compensatory expression of proteasome genes. WRR139 significantly potentiates the cytotoxicity of Carfilzomib against cancer cells, serving as a valuable tool for studying proteostasis and overcoming resistance to proteasome inhibitors.

WRR139
Cas No. 2138924-36-2
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$99-In Stock
5 mgPreferential-In Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
WRR139 is a peptide vinyl sulfone derivative that acts as a potent inhibitor of cytosolic N-glycanase 1 (NGLY1) and the transcription factor Nrf1. NGLY1-mediated deglycosylation is essential for the maturation and activation of Nrf1. By inhibiting NGLY1, WRR139 impairs Nrf1 processing, localization, and activation, thereby suppressing the compensatory expression of proteasome genes. WRR139 significantly potentiates the cytotoxicity of Carfilzomib against cancer cells, serving as a valuable tool for studying proteostasis and overcoming resistance to proteasome inhibitors.
In vitro
WRR139 (0.01-100 μM) inhibits NGLY1 and impairs Nrf1 processing [1].
WRR139 synergizes with Carfilzomib to enhance tumor cell cytotoxicity at 1 μM [1].
Chemical Properties
Molecular Weight456.6
FormulaC25H32N2O4S
Cas No.2138924-36-2
Smiles[C@@H](CCC1=CC=CC=C1)(NC(C=CS(=O)(=O)C2=CC=C(C)C=C2)=O)C(NCCC(C)C)=O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (175.21 mM), Sonication is recommmended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1901 mL10.9505 mL21.9010 mL109.5050 mL
5 mM0.4380 mL2.1901 mL4.3802 mL21.9010 mL
10 mM0.2190 mL1.0951 mL2.1901 mL10.9505 mL
20 mM0.1095 mL0.5475 mL1.0951 mL5.4753 mL
50 mM0.0438 mL0.2190 mL0.4380 mL2.1901 mL
100 mM0.0219 mL0.1095 mL0.2190 mL1.0951 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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