Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-

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Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- manufacturers
Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Basic information
Product Name:Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-
Synonyms:Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-;hSMG-1 inhibitor 11e;hSMG 1 inhibitor 11e,hSMG1 inhibitor 11e;hSMG-1 inhibitor 11e, 10 mM in DMSO
CAS:1402452-10-1
MF:C26H27N7O3S
MW:517.6
EINECS:
Product Categories:
Mol File:1402452-10-1.mol
Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Structure
Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Chemical Properties
storage temp. 4°C, away from moisture and light
solubility DMSO : 50 mg/mL (96.60 mM; Need ultrasonic)
form Solid
color White to light yellow
Safety Information
MSDS Information
Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Usage And Synthesis
UseshSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM)[1].
Biological ActivityHSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with IC50 value <0.05 nM. hSMG-1 inhibitor 11e exhibits 900-fold selectivity for hSMG-1 over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50 of 61 nM and 92 nM) and CDK1/CDK2 (IC50 of 32 μM and 7.1 μM).
in vitro

HSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment.

target

mTOR

45 nM (IC 50 )

PI3Kα

61 nM (IC 50 )

PI3Kγ

92 nM (IC 50 )

CDK1

32 μM ( IC 50 )

CDK2

7.1 μM (IC 50 )

hSMG-1

<0.05 nM (IC 50 )

IC 50hSMG-1: <0.05 nM (IC50); mTOR: 45 nM (IC50); PI3Kα: 61 nM (IC50); PI3Kγ: 92 nM (IC50); CDK1: 32 μM (IC50); CDK2: 7.1 μM (IC50)
References[1] Ariamala Gopalsamy, et al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41. DOI:10.1016/j.bmcl.2012.08.107
Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]- Preparation Products And Raw materials
Tag:Benzenesulfonamide, N,N,2-trimethyl-5-[[4-[2-[4-[[(methylamino)carbonyl]amino]phenyl]-4-pyridinyl]-2-pyrimidinyl]amino]-(1402452-10-1) Related Product Information
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