Nrf2 agonist C5

Chemical Structure : Nrf2 agonist C5

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货号: PC-24870Not For Human Use, Lab Use Only.

Nrf2 agonist C5 is a novel chalcone-derived covalent Keap1 binder and Nrf2 agonist, strongly blocks Keap1-Nrf2 interaction and enhances Nrf2 stability.

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生物&药学活性

Nrf2 agonist C5 is a novel chalcone-derived covalent Keap1 binder and Nrf2 agonist, strongly blocks Keap1-Nrf2 interaction and enhances Nrf2 stability.
C5 (0.5 μM) showed more potent Nrf2 agonist effects than SFN (10 μM) in HK-2 cells, a known Nrf2 agonist.
C5 could enhance Nrf2 stability and facilitated its nuclear translocation.
C5 (0.5-2 uM) significantly upregulated the transcriptional levels of the target genes of Nrf2, including HO-1, NQO1, GCLC and GCLM in HK-2 cells.
C5 activates Keap1/Nrf2 signaling via covalent modifying these two key cysteines of Keap1 (Cys288 and Cys319), thereby enhancing Nrf2 stability, promoting Nrf2 nuclear translocation and then activating the Keap1-Nrf2 signaling.
C5 ameliorates CDDP-induced kidney injury in HK-2 cells, C5 alleviates CDDP-induced mitochondrial damage.
C5 (5, 10, and 20 mg/kg/d) significantly ameliorates inflammatory injury in CIKI mice, dose-dependently attenuated renal inflammation, reducing pro-inflammatory cytokines (TNF-α, IL-1β and IL-6) in kidney tissues.

物理化学性质&存储条件

分子量	373.45
分子式	C24H23NO3
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	(E)-1-(2-hydroxy-6-methoxyphenyl)-3-(6-(pyrrolidin-1-yl)naphthalen-2-yl)prop-2-en-1-one

参考文献

1. Deng Y, et al. Redox Biol. 2025 Jun 21;85:103737.

Nrf2 agonist C5

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物理化学性质&存储条件

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Nrf2 agonist C5

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物理化学性质&存储条件

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