KI-696 (KI696) 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.KI-696 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).KI-696 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.KI-696 significantly reduces ozone-induced pulmonary inflammation, restores ozone-induced depletion of lung GSH levels in vivo.
Cat.No
DC70539
Name
KI-696
Chemical Properties
CAS
1799974-70-1
Formula
C28H30N4O6S
MW
550.63
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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