5.30838

NMD Inhibitor

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

• Synonim(y): 2-(((6,7-dimetylo-3-okso-1,2,3,4-tetrahydro-2-chinoksalinylo)acetylo)amino)-4,5-dimetylo-3-tiofenokarboksylan etylu, Nonsense-Mediated mRNA Decay Inhibitor 14, NMDI-14
• Wzór empiryczny (zapis Hilla): C₂₁H₂₅N₃O₄S
• Numer CAS: 307519-88-6
• Masa cząsteczkowa: 415.51
• Numer MDL: MFCD02073967
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Nazwa produktu: NMD Inhibitor,
• Próba: ≥95% (HPLC)
• Poziom jakości: 100
• Formularz: powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: yellow
• rozpuszczalność: DMSO: 10 mg/mL
• temp. przechowywania: −20°C
• ciąg 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)
• Klucz InChI: QRLPSNLBUMVXBL-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
SMG7

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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.

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable