SML3864
SMG1i
≥95% (HPLC), Potent and selective SMG-1 (hSMG-1; SMG1) kinase inhibitor, powder
Synonym(s):
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
Sign In to View Organizational & Contract Pricing.
Select a Size
About This Item
Empirical Formula (Hill Notation):
C27H28ClN7O3S
CAS Number:
Molecular Weight:
566.07
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Product Name
SMG1i, ≥95% (HPLC)
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Related Categories
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.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Choose from one of the most recent versions:
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Functional Restoration of CFTR Nonsense Mutations in Intestinal Organoids
Journal of Cystic Fibrosis, 21(2), 246-253 (2022)
Identification of pyrimidine derivatives as hSMG-1 inhibitors
Bioorganic & Medicinal Chemistry Letters, 22(21), 6636-6641 (2012)
Daniel R McHugh et al.
International journal of molecular sciences, 22(1) (2021-01-06)
Many heritable genetic disorders arise from nonsense mutations, which generate premature termination codons (PTCs) in transcribed mRNA. PTCs ablate protein synthesis by prematurely terminating the translation of mutant mRNA, as well as reducing mutant mRNA quantity through targeted degradation by
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service