SML2362

WRR139

≥98% (HPLC)

• 동의어(들): (S,E)-N-Isopentyl-4-phenyl-2-(3-tosylacrylamido)butanamide
• 실험식(Hill 표기법): C₂₅H₃₂N₂O₄S
• CAS Number: 2138924-36-2
• Molecular Weight: 456.60
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• 양식: powder
• 색상: white to beige
• solubility: DMSO: 2 mg/mL, clear
• 저장 온도: 2-8°C

설명

생화학적/생리학적 작용

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.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable