1402452-15-6

1402452-15-6 structure

Name: hSMG-1 inhibitor 11j
Chemical Name: compound 11j [PMID: 23021994]
CAS Number: 1402452-15-6
Molecular Formula: C₂₇H₂₈ClN₇O₃S
Molecular Weight: 566.074
Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
Create Date: 2018-06-11 07:24:22
Modify Date: 2024-01-07 09:25:37
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].

Name	compound 11j [PMID: 23021994]
Synonyms	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]-

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.