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Chemical Structure : KI-696
CAS No.: 1799974-70-1
Catalog No.: PC-38460Not For Human Use, Lab Use Only.
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $428 | In stock | |
| 50 mg | $1180 | In stock | |
| 100 mg | $1880 | In stock | |
| 1 g | Get quote |
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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.
| 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 |
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1. Thomas G Davies, et al. J Med Chem. 2016 Apr 28;59(8):3991-4006.
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