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G-1749

Chemical Structure : G-1749

CAS No.: 2245057-57-0

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G-1749 (G1749)

Catalog No.: PC-25599Not For Human Use, Lab Use Only.

G-1749 is a potent, very kinase-selective and allosteric activator of IRE1 RNase activity with EC50 of 9 nM in RNase biochemical assay.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

G-1749 is a potent, very kinase-selective and allosteric activator of IRE1 RNase activity with EC50 of 9 nM in RNase biochemical assay.
only 6 of 218 other kinases besides IRE1 by more than 50% at 1 uM.
G-1749 occupies a pocket proximal to the DFG motif.
G-1749 significantly increased the cellular levels of XBP1s mRNA and decreased those of DGAT2 in KMS-11 multiple myeloma cells.
G-1749 allosterically inhibits the RNase activity of phosphorylated IRE1
G-1749 stimulates the RNase activity of unphosphorylated IRE1 (IRE1-0P), yet inhibits IRE1-3P.

Physicochemical Properties

M.Wt 498.59
Formula C28H30N6O3
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

ethyl (S)-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)carbamate

References

1. Ferri E, et al. Nat Commun. 2020 Dec 14;11(1):6387.

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