TN5171
|
|
|
Apoptosis
Others
Nrf2
|
Tricetin 是一种从石榴中分离出的类黄酮。Tricetin 是 Keap1-Nrf2 蛋白相互作用(PPI)的强效竞争性抑制剂,通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路,保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1(PS-1)表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症,保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。 |
T6S0525
|
|
|
ERK
p38 MAPK
Akt
|
Farrerol 是一种杜鹃花的生物活性成分,具有抗氧化、抗肿瘤、抗炎、神经保护和肝保护等多种功能。 |
T27077
|
|
|
|
CPUY192018 Disodium is a potent inhibitor of the Keap1-Nrf2 PPI. The inhibition of the Keap1-Nrf2 PPI may be beneficial as a treatment for ulcerative colitis. |
T78841
|
|
|
|
Nrf2-IN-3 (Compound R16) 为Nrf2抑制剂,与KEAP1突变体 (G333C mKEAP1) 结合,能够恢复受损的KEAP1/NRF2相互作用。该化合物通过修复mKEAP1/NRF2复合物,增加KEAP1突变癌细胞对Cisplatin和Gefitinib的敏感性。 |
T22556
|
|
|
Others
|
Nrf2/Keap1 and Keap1/Cul3 interaction inhibitor |
T69401
|
|
|
|
MIND4-17为一种NRF2激活剂,通过共价修饰Keap1的C151残基发挥作用。该化合物能破坏Keap1-Nrf2之间的结合,进而促进Nrf2蛋白的稳定性及其向核内的迁移,显示出显著的抗氧化活性。 |
T75914
|
|
|
|
TAT-14 TFA,一种作为Nrf2激活因子的14聚体肽,不影响Nrf2 mRNA的表达,而是通过靶向Nrf2上Keap1的结合位点来提升Nrf2蛋白水平。 |
T73205
|
|
|
|
Praelolide是一种有效的Nrf2激活剂,能够抑制破骨细胞的生成与活性氧(ROS)的产生,并通过与Keap1的非共价结合,破坏Keap1-Nrf2蛋白质-蛋白质相互作用。因此,Praelolide展现出在破骨细胞性骨病研究中的应用潜力。 |
T79698
|
|
|
|
S217879是一种选择性高效的NRF2激活剂,能够破坏KEAP1-NRF2之间的相互作用,从而强有力地激活NRF2通路。它可应用于非酒精性脂肪性肝炎(NASH)的研究领域。 |
T36614
|
|
|
|
Nrf2 activation of the antioxidant response element (ARE) is central to cytoprotective gene expression against oxidative and/or electrophilic stress. Unless activated by inflammatory, environmental, or oxidative stressors, Nrf2 is sequestered in the cytoplasm by its repressor, Keap1. Because of its protective capabilities, small molecules that activate Nrf2 signaling are being examined as potential anti-cancer or anti-inflammatory agents. DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC) is a major metabolite of SFN , a powerful inducer of chemopreventative enzymes via Keap1-Nrf2 signaling and ARE-driven gene expression. At 75 μM, SFN-NAC has been shown to increase ARE expression in HepG2-C8 cells. Its reported potency on ARE-related gene expression is roughly 8-fold less than SFN. |