SML3618
KI-696
≥98% (HPLC)
别名:
(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, (3S)-3-(7-Methoxy-1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(4-methyl-3-(((R)-4-methyl-1,1-dioxido-3,4-dihydro-2H-benzo[b]-[1,4,5]oxathiazepin-2-yl)methyl)phenyl)propanoic acid, KI 696, KI696
登录查看公司和协议定价
所有图片(1)
About This Item
生化/生理作用
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.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Thomas G Davies et al.
Journal of medicinal chemistry, 59(8), 3991-4006 (2016-04-01)
KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress. Pharmacological intervention has focused on molecules that decrease NRF2-ubiquitination through covalent modification of KEAP1 cysteine residues, but such electrophilic
[Treatment of acute thromboembolism in hereditary antithrombin deficiency--a review].
L Tengborn
Lakartidningen, 84(15), 1249-1251 (1987-04-08)
Patrizia Romani et al.
Nature cell biology, 24(2), 168-180 (2022-02-16)
Metastatic breast cancer cells disseminate to organs with a soft microenvironment. Whether and how the mechanical properties of the local tissue influence their response to treatment remains unclear. Here we found that a soft extracellular matrix empowers redox homeostasis. Cells
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系技术服务部门