KI-696，5MG，SML3618-5MG，Sigma

Biochem/physiol Actions

KI-696 is a non-cytotoxic (10 mM; BEAS-2B cells), Kelch domain-targeing (Kd ~1.3 nM) KEAP1 selective inhibitor that effectively upregulates nuclear NRF2 level in NHBE cells (%increase/[KI-696] = 100%/10 nM and 127%/100 nM; 6 hr) and NRF2 target genes transcription by blocking KEAP1-mediated NRF2 downregulation. KI-696 (5-50 mmol/kg i.v.) upregulates NRF2 target genes transcription in rat lungs in vivo, as well as alleviate ozone-induced pulmonary inflammation and GSH depletion. KI-696 inhibits OATP1B1, BSEP, and PDE3A only at much higher concentrations (IC50 = 2.5, 4.0, 10 mM, respectively) and exhibits little or no potency toward a panel of 46 channels, enzymes, and receptors.
Non-cytotoxic, selective KEAP1 Kelch domain inhibitor that effectively upregulates NRF2 actfivity in cultures and in rats in vivo.