SML3864

SMG1i

≥95% (HPLC), Potent and selective SMG-1 (hSMG-1; SMG1) kinase inhibitor, powder

• Sinonimo/i: 1-[4-[4-[2-[4-Chloro-3-(diethylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea, 2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]benzenesulfonamide, NMDi, SMG1 inhibitor 11j, SMG1 inhibitor compound 11j
• Formula empirica (notazione di Hill): C₂₇H₂₈ClN₇O₃S
• Numero CAS: 1402452-15-6
• Peso molecolare: 566.07
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD30186925
• Assay: ≥95% (HPLC)
• Form: powder

Proprietà

• Nome del prodotto: SMG1i, ≥95% (HPLC)
• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Descrizione

Biochem/physiol Actions

Potent and selective SMG-1 (hSMG-1; SMG1) kinase inhibitor that blocks nonsense-mediated decay (NMD).


SMG1i is a potent and selective SMG-1 kinase inhibitor (hSMG-1 IC50 = 110 pM) with much reduced potency against mTOR, PI3Kα/γ and CDK1/2 (IC50 = 50 nM, 92/60 nM, 32/7.1 μM, respectively). SMG1i selectively downregulates MDA361 cellular phosphorylation of UPF1 (0.3 -1 μM), but not that of mTOR or AKT substrates (p70s6 K and PI3K). Nonsense-mediated decay (NMD) inhibition by SMG1i (1 µM) is shown to synergize with premature termination codons (PTCs) readthrough agents (G418, gentamicin, and paromomycin) in promoting the expression of CFTR protein in murine cells carrying Cftr G542X nonsense mutation.

Informazioni sulla sicurezza

• Classe di stoccaggio: 11 - Combustible Solids
• WGK: WGK 3
• Punto di infiammabilità (°F): Not applicable
• Punto di infiammabilità (°C): Not applicable