5.30838

NMD Inhibitor

≥95% (HPLC), powder, NMD inhibitor, Calbiochem^®

• Sinónimos: NMD Inhibitor, Ethyl 2-(((6,7-dimethyl-3-oxo-1,2,3,4-tetrahydro-2-quinoxalinyl)acetyl)amino)-4,5-dimethyl-3-thiophenecarboxylate, Nonsense-Mediated mRNA Decay Inhibitor 14, NMDI-14
• Fórmula empírica (notación de Hill): C₂₁H₂₅N₃O₄S
• Número de CAS: 307519-88-6
• Peso molecular: 415.51
• Número MDL: MFCD02073967
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nombre del producto: NMD Inhibitor,
• Ensayo: ≥95% (HPLC)
• Nivel de calidad: 100
• Formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 10 mg/mL
• temp. de almacenamiento: −20°C
• cadena SMILES: [s]1c(c(c(c1C)C)C(=O)OCC)NC(=O)CC2Nc3c(cc(c(c3)C)C)NC2=O
• InChI: 1S/C21H25N3O4S/c1-6-28-21(27)18-12(4)13(5)29-20(18)24-17(25)9-16-19(26)23-15-8-11(3)10(2)7-14(15)22-16/h7-8,16,22H,6,9H2,1-5H3,(H,23,26)(H,24,25)
• Clave InChI: QRLPSNLBUMVXBL-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable tetrahydroquinoxalinyl-thiophenecarboxylate compound that inhibits nonsense-mediated mRNA decay (NMD) in a dose-dependent manner and enhances the stability of premature termination codon (PTC) mutated p53 mRNA in N417 and HDQP-1 cells. However, it does not affect the stability of wild-type p53 in U2OS cells. Shown to dock reversibly within a SMG7 pocket and disrupt SMG7-UPF1 interaction and prevent their complex formation. Acts synergistically with G418 (Cat. No. 345810; 200 µg/ml) to increase p53 expression in p53 PTC mutant cells leading to increase mRNA levels of p21, Bax, and PUMA. Does not display any toxicity (>50 µM) in multiple cell lines and has no effect on proliferation and protein synthesis in transformed and non-transformed cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
SMG7

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Use only fresh DMSO for reconstitution.

Otras notas

Martin, L., et al. 2014. Cancer Res.74, 3104.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable