KI696 (Ki696, KI-696)

Chemical Structure : KI696

CAS No.: 1799974-70-1

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货号: 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.

规格	价格	库存
1 mg	￥1280	In stock
5 mg	￥2180	In stock
10 mg	￥3580	In stock
25 mg	￥5880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	550.63
分子式	C28H30N4O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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