Chemical Structure : hSMG-1 inhibitor 11j
CAS No.: 1402452-15-6
Catalog No.: PC-35721Not For Human Use, Lab Use Only.
hSMG-1 inhibitor 11j (SMG1i) is a potent, selective PI3K-related protein kinase hSMG-1 inhibitor with IC50 of 0.11 nM, 455-fold selectivity over mTOR and no activity against CDK1/2.
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hSMG-1 inhibitor 11j (SMG1i) is a potent, selective PI3K-related protein kinase hSMG-1 inhibitor with IC50 of 0.11 nM, 455-fold selectivity over mTOR and no activity against CDK1/2.
SMG1i eliminates UPF1 phosphorylation at 1 uM and significantly reduced it at 0.3 uM, shows little apparent effect on phospho p70s6 K and phospho AKT, targets of mTOR and PI3K.
SMG1i specifically inhibits SMG1 in vitro by competing with ATP binding.
SMG1i also shows good inhibition in an MDA468 cell proliferation assay with an IC50 of 75 nM, providing a tool compound to probe hSMG-1 mediated tumor biology.
M.Wt | 566.077 | |
Formula | C27H28ClN7O3S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
2-chloro-N,N-diethyl-5-((4-(2-(4-(3-methylureido)phenyl)pyridin-4-yl)pyrimidin-2-yl)amino)benzenesulfonamide |
1. Gopalsamy A, et al. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41.
2. Lukas M Langer, et al. Elife. 2021 Oct 26;10:e72353.
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