WRR139

WRR139

Biochem/physiol Actions

WRR139 is a peptidyl vinyl sulfone that inhibits NGLY1 (N-glycanase 1; PNGase; Peptide-N(4)-(N-acetyl-beta-glucosaminyl)asparagine amidase) de-N-glycosylation activity in cell-free enzymatic assays (IC50 <10 μM; 3.75 rhNGLY1 wtih 1.7 μg S-alkylated RNase B as substrate) and in cultures (IC50 = 5.5 μM in ddVenus reporter K562 cells co-treated with 1 μM proteasome inhibitor carfilzomib). WRR139 disrupts NGLY1-mediated nuclear respiratory factor 1 (NRF1) processing/activation. WRR139 (1 μM) is shown to potentiate the cytotoxicity of proteasome inhibitor carfilzomib (1-100 nM) in multiple myeloma (MM; U266 & H929), T-cell acute lymphoblastic leukemia (T-ALL; Jurkat), and HeLa cultures, but not in NGLY1-knockdown HeLa cells. Note: concentrations below 10 μM is generally recommended for culture treatment to avoid off-target activity against caspases.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576206 WRR139 white to beige SIGMA-ALDRICH 2-8&deg;C DMSO: 2 mg/mL, clear powder &ge;98% (HPLC)
£727.07 (exc VAT) per EACH
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3576207 WRR139 white to beige SIGMA-ALDRICH 2-8&deg;C DMSO: 2 mg/mL, clear powder &ge;98% (HPLC)
£240.96 (exc VAT) per EACH
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