Chemical Structure : KI696
CAS No.: 1799974-70-1
Catalog No.: PC-38460Not For Human Use, Lab Use Only.
KI696 (Ki696, KI-696) is a highly potent, selective inhibitor of KEAP1-NRF2 interaction, exhibits very high affinity for the KEAP1 Kelch domain with ITC Kd of 1.3 nM.
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KI696 (Ki696, KI-696) is a highly potent, selective inhibitor of KEAP1-NRF2 interaction, exhibits very high affinity for the KEAP1 Kelch domain with ITC Kd of 1.3 nM.
KI696 displays high selectivity against a panel of 49 in vitro functional assays for targets, with the exception of the OATP1B1 (IC50=2.5 µM), the bile salt export pump BSEP (IC50=4.0 µM), and PDE3A (IC50=10 uM).
KI696 increases NRF2 nuclear translocation in normal human bronchial epithelial cells, up-regulates NRF2-dependent gene expression NQO1 and GCLM, and increases NQO1 activity in an NRF2-dependent manner.
KI696 significantly reduces ozone-induced pulmonary inflammation, restores ozone-induced depletion of lung GSH levels in vivo.
M.Wt | 550.63 | |
Formula | C28H30N4O6S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(βS)-β-[3-[[(4R)-3,4-Dihydro-4-methyl-1,1-dioxido-2H-5,1,2-benzoxathiazepin-2-yl]methyl]-4-methylphenyl]-7-methoxy-1-methyl-1H-benzotriazole-5-propanoic acid |
1. Thomas G Davies, et al. J Med Chem. 2016 Apr 28;59(8):3991-4006.
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