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GSK3227634

Chemical Structure : GSK3227634

CAS No.: 1799977-30-2

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GSK3227634 (GSK-3227634)

Catalog No.: PC-28126Not For Human Use, Lab Use Only.

GSK3227634 is a potent, ultrahigh-affinity, noncovalent, reversible inhibitor of KEAP1-NRF2 (SPR pKd=10.9, TR-FRET pIC50=9.0) and NRF2 activator.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK3227634 is a potent, ultrahigh-affinity, noncovalent, reversible inhibitor of KEAP1-NRF2 (SPR pKd=10.9, TR-FRET pIC50=9.0) and NRF2 activator.
GSK3227634 activates the NRF2 pathway both in vitro in human lung epithelial cells as well as in vivo after intratracheal administration in a rat model of lung oxidative stress.

Physicochemical Properties

M.Wt 563.67
Formula C29H33N5O5S
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

(S)-3-(3-(((R)-4-Ethyl-1,1-dioxido-3,4-dihydro-2H-pyrido[2,3-b][1,4,5]oxathiazepin-2-yl)methyl)-4-methylphenyl)-3-(1-ethyl-4-methyl-1H-benzo[d][1,2,3]triazol-5-yl)propanoic acid

References

1. Callahan JF, et al. J Med Chem. 2026 Sep 10;69(17):20859-20876.

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