5.30838

NMD Inhibitor

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

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₁H₂₅N₃O₄S
• CAS-Nummer: 307519-88-6
• Molekulargewicht: 415.51
• MDL-Nummer: MFCD02073967
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Produktbezeichnung: NMD Inhibitor,
• Assay: ≥95% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: yellow
• Löslichkeit: DMSO: 10 mg/mL
• Lagertemp.: −20°C
• SMILES String: [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)
• InChIKey: QRLPSNLBUMVXBL-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
SMG7

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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.

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable