NGLY1 (N-glycanase 1; PNGase) inhibitor that disrupts NGLY1-mediated NRF1 activation and potentiates carfilzomib cytotoxicity in cancer cultures.
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.
The Proteasome Inhibitor Set I controls the biological activity of Proteasome. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
form
powder
form
lyophilized powder
form
buffered aqueous glycerol solution
form
solid
assay
≥98% (HPLC)
assay
-
assay
-
assay
-
storage temp.
2-8°C
storage temp.
−20°C
storage temp.
−20°C
storage temp.
−20°C
solubility
DMSO: 2 mg/mL, clear
solubility
-
solubility
-
solubility
-
color
white to beige
color
-
color
-
color
-
Storage Class
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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