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hSMG-1 inhibitor 11j

Names

[ CAS No. ]:
1402452-15-6

[ Name ]:
hSMG-1 inhibitor 11j

[Synonym ]:
compound 11j [PMID: 23021994]
2-Chloro-N,N-diethyl-5-{[4-(2-{4-[(methylcarbamoyl)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]-

Biological Activity

[Description]:

hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer[1].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR
Signaling Pathways >> Stem Cell/Wnt >> GSK-3
Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

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)


[In Vitro]

hSMG-1 inhibitor 11j (0.3-3 μM; 6 h) significantly reduces UPF1 phosphorylation at 0.3 μM, and eliminates it at 1 μM in MDA 361 cells[1]. hSMG-1 inhibitor 11j inhibits MDA468 cell proliferation, with an IC50 of 75 nM[1].

[References]

[1]. Gopalsamy A, et, al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C27H28ClN7O3S

[ Molecular Weight ]:
566.074

[ Exact Mass ]:
565.166260

[ LogP ]:
4.38

[ Index of Refraction ]:
1.640

Related Compounds