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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.

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $99 | - | In Stock | |
| 5 mg | Preferential | - | In Stock |
| 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]. |
| Molecular Weight | 456.6 |
| Formula | C25H32N2O4S |
| 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 | Powder: -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
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. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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