5.30838

NMD Inhibitor

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₁H₂₅N₃O₄S
• CAS Number: 307519-88-6
• Molecular Weight: 415.51
• UNSPSC Code: 12352200

Properties

• Assay: ≥95% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 10 mg/mL
• storage temp.: −20°C

Description

General description

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.

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 Actions

Cell permeable: yes

Primary Target
SMG7

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Other Notes

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

Legal Information

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

Safety Information

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