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Description: KI-696 is a novel and high affinity chemical probe for KEAP1 and a potent inhibitor that can disrupt the KEAP1/NRF2 protein-protein interaction. KI-696 represents an excellent probe to study the KEAP1-NRF2 interaction in vivo. Discovered by FBS, the probe is well characterised in a number of in vitro assays as well as showing robust in vivo effects. The in vivo application is hampered by low bioavailability and high clearance, necessitating IV infusions as the mode of administration, which may limit the usefulness of the probe in vivo.
References: MonoacidicInhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear FactorErythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interactionwith High Cell Potency Identified by Fragment-Based Discovery. J MedChem. 2016 Apr 28; 59(8):3991-4006.
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