SML2362

WRR139

≥98% (HPLC)

• 别名: (S,E)-N-Isopentyl-4-phenyl-2-(3-tosylacrylamido)butanamide
• 经验公式（希尔记法）: C₂₅H₃₂N₂O₄S
• CAS号: 2138924-36-2
• 分子量: 456.60
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: white to beige
• 溶解度: DMSO: 2 mg/mL, clear
• 儲存溫度: 2-8°C

说明

生化／生理作用

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.

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable