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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 microg/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 microM) 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., 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 microg/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 microM) in multiple cell lines and has no effect on proliferation and protein synthesis in transformed and non-transformed cells.

Strukturformel

SAF-5308380001

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