ChemicalBook > CAS DataBase List > 2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide

2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide

Product Name
2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide
CAS No.
1402452-15-6
Chemical Name
2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide
Synonyms
SMG1i;ap261133;hSMG-1 inhibitor 11j;Pyrimidine Related Compound 1;hSMG 1 inhibitor 11j,hSMG1 inhibitor 11j;2-Chloro-N,N-diethyl-5-((4-(2-(4-(3-methylureido)phenyl)pyridin-4-yl)pyrimidin-2-yl)amino)benzenesulfonamide;2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide;Benzenesulfonamide, 2-chloro-N,N-diethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-
CBNumber
CB12695063
Molecular Formula
C27H28ClN7O3S
Formula Weight
566.07
MOL File
1402452-15-6.mol
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2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide Property

Density 
1.353±0.06 g/cm3(Predicted)
storage temp. 
4°C, away from moisture and light
solubility 
DMSO: 2mg/mL, clear
form 
Solid
pka
14.00±0.46(Predicted)
color 
White to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3864
Product name
SMG1i
Purity
≥95% (HPLC)
Packaging
5 mg
Price
$474.05
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3864
Product name
SMG1i
Purity
≥95% (HPLC)
Packaging
10 mg
Price
$899
Updated
2025/07/31
TRC
Product number
C421860
Product name
2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]benzenesulfonamide
Packaging
25mg
Price
$1760
Updated
2021/12/16
ChemScene
Product number
CS-0087425
Product name
hSMG-1inhibitor11j
Purity
98.91%
Packaging
5mg
Price
$500
Updated
2021/12/16
ChemScene
Product number
CS-0087425
Product name
hSMG-1inhibitor11j
Purity
98.91%
Packaging
10mg
Price
$850
Updated
2021/12/16
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2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide Chemical Properties,Usage,Production

Uses

2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]benzenesulfonamide are pyrimidine derivatives as hSMG-1 inhibitors.

Biological Activity

Potent and selective SMG-1 (hSMG-1; SMG1) kinase inhibitor th at 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 th at 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.

IC 50

hSMG-1: 0.11 nM (IC50); mTOR: 50 nM (IC50); PI3Kγ: 60 nM (IC50); PI3Kα: 92 nM (IC50); GSKα: 260 (IC50); GSKβ: 330 (IC50); CDK2: 7.1 μM (IC50); CDK1: 32 μM (IC50)

2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide Preparation Products And Raw materials

Raw materials

Preparation Products

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2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide Suppliers

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1402452-15-6, 2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMideRelated Search:


  • 2-Chloro-N,N-diethyl-5-[[4-[2-[4-[[(MethylaMino)carbonyl]aMino]phenyl]-4-pyridinyl]-2-pyriMidinyl]aMino]benzenesulfonaMide
  • Pyrimidine Related Compound 1
  • ap261133
  • Benzenesulfonamide, 2-chloro-N,N-diethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-
  • hSMG-1 inhibitor 11j
  • hSMG 1 inhibitor 11j,hSMG1 inhibitor 11j
  • 2-Chloro-N,N-diethyl-5-((4-(2-(4-(3-methylureido)phenyl)pyridin-4-yl)pyrimidin-2-yl)amino)benzenesulfonamide
  • SMG1i
  • 1402452-15-6
  • C27H28ClN7O3S
  • Amines, Aromatics, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds