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hSMG-1 inhibitor 11j

Chemical Structure : hSMG-1 inhibitor 11j

CAS No.: 1402452-15-6

hSMG-1 inhibitor 11j (SMG1i)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 566.077
Formula C27H28ClN7O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-chloro-N,N-diethyl-5-((4-(2-(4-(3-methylureido)phenyl)pyridin-4-yl)pyrimidin-2-yl)amino)benzenesulfonamide

References

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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