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SML3864

Sigma-Aldrich

SMG1i

≥95% (HPLC)

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

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About This Item

Empirical Formula (Hill Notation):
C27H28ClN7O3S
CAS Number:
Molecular Weight:
566.07
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Identification of pyrimidine derivatives as hSMG-1 inhibitors
Bioorganic & Medicinal Chemistry Letters, 22(21), 6636-6641 (2012)
Functional Restoration of CFTR Nonsense Mutations in Intestinal Organoids
Journal of Cystic Fibrosis, 21(2), 246-253 (2022)
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

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