KEAP1-Nrf2
The KEAP1-Nrf2 pathway is the major regulator of cytoprotective responses to chemical and/or oxidative stresses caused by reactive oxygen species (ROS) and electrophiles. Nrf2 (nuclear factor erythroid 2-related factor 2) is a transcription factor that binds together with small Maf proteins to the antioxidant response element (ARE) in the regulatory regions of cellular defense enzyme genes leading to the activation of a wide rang of cell defense processes; while KEAP1 (Kelch ECH associating protein 1), a negative repressor of Nrf2, is an adaptor protein for a Cul3-based ubiqutitin E3 ligase that binds to Nrf2 and promotes its degradation by the ubiquitin proteasome pathway.
- Cat.No. 产品名称 Information
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GN10654
(+)-Corynoline
An isoquinoline alkaloid with diverse biological activities
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GC31691
(+)-DHMEQ
(+)-DHMEQ 是抗氧化转录因子 Nrf2 的激活剂。
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GC65610
(R)-5-Hydroxy-1,7-diphenyl-3-heptanone
(R)-5-Hydroxy-1,7-diphenyl-3-heptanone 是一种二芳基庚烷,存在于 Alpinia officinarum 中。(R)-5-Hydroxy-1,7-diphenyl-3-heptanone 通过激活 Nrf2/ARE 通路改善氧化应激和胰岛素抵抗。
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GC15355
2-Trifluoromethyl-2'-methoxychalcone
A potent activator of Nrf2
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GC33815
4-Hydroxyphenylacetic acid
A phenolic acid with anti-inflammatory and anti-steatotic activities
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GC31648
4-Octyl Itaconate
4-Octyl Itaconate 是一种可渗透细胞的衣康酸酯衍生物。
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GN10629
5,7-dihydroxychromone
A flavone decomposition product with diverse biological activities
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GC16120
AI-3
Nrf2/Keap1 and Keap1/Cul3 interaction inhibitor
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GN10415
Astilbin
A flavonoid with diverse biological activities
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GC15371
Bardoxolone
An anti-inflammatory compound that activates Nrf2/ARE signaling
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GC11572
Bardoxolone methyl
A synthetic triterpenoid with potent anticancer and antidiabetic activity
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GC34070
Brusatol (NSC 172924)
A quassinoid with diverse biological activities
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GC61636
CBR-470-2
CBR-470-2是甘氨酸取代的类似物,可以激活NRF2信号传导。CBR-470-2可用于调节糖酵解。
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GC35629
CDDO-dhTFEA
CDDO-dhTFEA (RTA dh404) 是一种合成的齐墩果烷三萜化合物,有效激活 Nrf2 并抑制促炎转录因子 NF-κB。 CDDO-dhTFEA 可以恢复高血压 (MAP),增加 Nrf2 及其靶基因的表达,减弱 NF-κB 的活化和转化生长因子-β 途径,并减少慢性肾病 (CKD) 大鼠的肾小球硬化,间质纤维化和炎症。
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GC35630
CDDO-EA
CDDO-EA 是一种 NF-E2 相关因子 2 /抗氧化反应元件 (Nrf2/ARE) 激活剂。
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GC32723
CDDO-Im (RTA-403)
An activator of Nrf2 signaling
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GC14787
Curcumin
A yellow pigment with diverse biological activities
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GC40226
Curcumin-d6
An internal standard for the quantification of curcumin
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GN10318
Danshensu
A salvianolic acid with diverse biological activities
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GC34010
Danshensu (Dan shen suan A)
Danshensu是丹参的有效成分,能够激活Nrf2信号通路,保护心血管。
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GC64971
DDO-7263
DDO-7263 是一种 1,2,4-Oxadiazole 衍生物,是一种有效的 Nrf2-ARE 激活剂。DDO-7263 通过与 Rpn6 结合上调 Nrf2,从而阻断 26S 蛋白酶体的组装和随后泛素化 Nrf2 的降解。DDO-7263 诱导 Nrf2 易位进入细胞核。DDO-7263 抑制 NLRP3 炎性体激活。DDO-7263 具有抗炎活性,并且有潜力用于神经退行性疾病(例如帕金森病 (PD)) 的研究。
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GC61419
Dibenzoylmethane
Dibenzoylmethane是甘草中的次要成分,可激活Nrf2并预防各种癌症和氧化损伤。Dibenzoylmethane是姜黄素的类似物,会引起Keap1解离和Nrf2的核易位。
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GC16590
Dimethyl Fumarate
An antioxidant with immunological actions
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GC62936
Dimethyl fumarate D6
Dimethyl fumarate D6 是 Dimethyl fumarate 的氘代标记物。Dimethyl fumarate 是一种 Nrf2 激活剂,能够诱导上调抗氧化基因的表达。
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GN10531
Dimethylfraxetin
A coumarin with anti-inflammatory activity
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GN10470
Eriodictyol
圣草酚是一种从中药中分离出来的黄酮类化合物,具有抗氧化和抗炎活性。
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GC62957
Eriodictyol-7-O-glucoside
A flavanone glucoside with diverse biological activities
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GC15605
Ezetimibe
A cholesterol transport inhibitor
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GC60159
Ezetimibe ketone
Ezetimibe ketone (EZM-K) 是 Ezetimibe 的 I 期代谢产物。Ezetimibe 是一种 NPC1L1 抑制剂,是有效的 Nrf2 激活剂,Ezetimibe 还是有效的胆固醇吸收抑制剂。
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GC66354
Ezetimibe-d4-1
An internal standard for the quantification of ezetimibe
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GN10741
Garcinone D
A xanthone with diverse biological activities
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GN10038
Ginsenoside Rh3
Ginsenoside Rh3 是 Ginsenoside Rg5 的细菌代谢产物。
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GC33092
Hesperin
An isothiocyanate with diverse biological activities
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GC11302
Hinokitiol
A tropolone with diverse biological activities
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GC66004
K67
K67 特异性抑制 Keap1 和 S349磷酸化 p62 之间的相互作用。K67 抑制 p-p62 与 Keap1 的竞争性结合,通过恢复 Keap1 驱动的 Nrf2 泛素化降解,有效抑制高表达S351磷酸化 p62 的 HCC 细胞的增殖。
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GC36390
Keap1-Nrf2-IN-1
Keap1–Nrf2 IN-1 (compound35) 是一种 Keap1- nrf2 蛋白-蛋白相互作用抑制剂,对 Keap1 蛋白作用的 IC50 值为 43 nM。Keap1–Nrf2 IN-1 (compound35) 能激活 Nrf2 调节的细胞保护反应,并在细胞和体内模型中对乙酰氨基酚诱导的肝损伤产生拮抗作用。
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GC31321
KI696
KI696是一种干扰Keap1/NRF2相互作用的高亲和力探针。
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GC34642
KI696 isomer
KI696isomer是KI696的低活性异构体。KI696是一种高亲和力探针,可破坏Keap1/NRF2相互作用。
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GC44006
Kinsenoside
A glycoside with diverse biological activities
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GN10491
Mangiferin
A xanthone glucoside with diverse biological activities
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GC31783
Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester)
Methyl protocatechuate (Methyl 3,4-dihydroxybenzoate, 3,4-Dihydroxybenzoic acid methyl ester, Protocatechuic Acid Methyl Ester) is also known as Protocatechuic Acid Methyl Ester. Protocatechuic Acid, a dihydroxybenzoic acid, is a major metabolite of antioxidant polyphenols found in green tea with antioxidant and anti-inflammatory effects.
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GC38819
ML334
An inhibitor of the Nrf2-Keap1 protein-protein interaction
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GC19254
ML385
An inhibitor of Nrf2
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GC13058
NK 252
A Nrf2 activator
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GC69590
Nrf2 activator-2
Nrf2 activator-2 (compound O15) 是一种蛇床子素衍生物,一种有效的 Nrf2 激动剂,在 293 T 细胞中的 EC50 为 2.9 μM。Nrf2 activator-2有效抑制 Keap1 和 Nrf2 的相互作用,从而显示出对 Nrf2 的激活作用。Nrf2 activator-2 显示细胞中泛素化 Nrf2 水平显着降低。
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GC66054
Nrf2 activator-4
Nrf2 activator-4 (Compound 20a) 是一种高效的、具有口服活性的 Nrf2 激活剂,EC50 值为 0.63 µM。Nrf2 activator-4 抑制小神经胶质细胞中活性氧 (reactive oxygen species) 的产生。Nrf2 activator-4 在 scopolamine 诱导的小鼠模型中能有效地恢复学习和记忆损伤。
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GC36773
Nrf2-IN-1
Nrf2-IN-1 (Compound 4f) 是 Nrf2 的抑制剂,具有作为治疗急性髓性白血病 (AML) 药物的前景。
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GC12821
Oltipraz
A Nrf2 and CAR activator
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GC13693
Omaveloxolone (RTA-408)
A synthetic triterpenoid that blocks Keap1/Nrf2 signaling
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GC15457
Pyridoxine
A 4-methanol form of vitamin B6