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Home >> Signaling Pathways >> Immunology/Inflammation >> KEAP1-Nrf2

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.

  1. Cat.No. 产品名称 Information
  2. GN10654 (+)-Corynoline An isoquinoline alkaloid with diverse biological activities
  3. GC31691 (+)-DHMEQ (+)-DHMEQ 是抗氧化转录因子 Nrf2 的激活剂。
  4. 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。
  5. GC15355 2-Trifluoromethyl-2'-methoxychalcone A potent activator of Nrf2
  6. GC33815 4-Hydroxyphenylacetic acid A phenolic acid with anti-inflammatory and anti-steatotic activities
  7. GC31648 4-Octyl Itaconate

    4-Octyl Itaconate 是一种可渗透细胞的衣康酸酯衍生物。
  8. GN10629 5,7-dihydroxychromone A flavone decomposition product with diverse biological activities
  9. GC16120 AI-3 Nrf2/Keap1 and Keap1/Cul3 interaction inhibitor
  10. GN10415 Astilbin A flavonoid with diverse biological activities
  11. GC15371 Bardoxolone An anti-inflammatory compound that activates Nrf2/ARE signaling
  12. GC11572 Bardoxolone methyl A synthetic triterpenoid with potent anticancer and antidiabetic activity
  13. GC34070 Brusatol (NSC 172924) A quassinoid with diverse biological activities
  14. 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。
  15. 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。
  16. 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。
  17. GC32723 CDDO-Im (RTA-403) An activator of Nrf2 signaling
  18. GC14787 Curcumin A yellow pigment with diverse biological activities
  19. GC40226 Curcumin-d6 An internal standard for the quantification of curcumin
  20. GN10318 Danshensu A salvianolic acid with diverse biological activities
  21. 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。
  22. 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。
  23. 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。
  24. GC16590 Dimethyl Fumarate An antioxidant with immunological actions
  25. 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。
  26. GN10531 Dimethylfraxetin A coumarin with anti-inflammatory activity
  27. 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。
  28. GC62957 Eriodictyol-7-O-glucoside A flavanone glucoside with diverse biological activities
  29. GC15605 Ezetimibe A cholesterol transport inhibitor
  30. 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。
  31. GC66354 Ezetimibe-d4-1 An internal standard for the quantification of ezetimibe
  32. GN10741 Garcinone D A xanthone with diverse biological activities
  33. GN10038 Ginsenoside Rh3 Ginsenoside Rh3 是 Ginsenoside Rg5 的细菌代谢产物。
  34. GC33092 Hesperin An isothiocyanate with diverse biological activities
  35. GC11302 Hinokitiol A tropolone with diverse biological activities
  36. 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。
  37. 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。
  38. GC31321 KI696 KI696是一种干扰Keap1/NRF2相互作用的高亲和力探针。
  39. 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。
  40. GC44006 Kinsenoside A glycoside with diverse biological activities
  41. GN10491 Mangiferin A xanthone glucoside with diverse biological activities
  42. 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.
  43. GC38819 ML334 An inhibitor of the Nrf2-Keap1 protein-protein interaction
  44. GC19254 ML385

    An inhibitor of Nrf2
  45. GC13058 NK 252 A Nrf2 activator
  46. 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。
  47. 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。
  48. 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。
  49. GC12821 Oltipraz A Nrf2 and CAR activator
  50. GC13693 Omaveloxolone (RTA-408) A synthetic triterpenoid that blocks Keap1/Nrf2 signaling
  51. GC15457 Pyridoxine A 4-methanol form of vitamin B6

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