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KI696

Chemical Structure : KI696

CAS No.: 1799974-70-1

KI696 (Ki696, KI-696)

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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1 mg $128 In stock
5 mg $218 In stock
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25 mg $588 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 550.63
Formula C28H30N4O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

1. Thomas G Davies, et al. J Med Chem. 2016 Apr 28;59(8):3991-4006.

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