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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. 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。
  3. GC25351 Dimethyl itaconate Dimethyl itaconate can reprogram neurotoxic to neuroprotective primary astrocytes through the regulation of LPS-induced Nod-like receptor protein 3 (NLRP3) inflammasome and nuclear factor 2/heme oxygenase-1 (NRF2/HO-1) pathways.
  4. GC66354 Ezetimibe-d4-1 An internal standard for the quantification of ezetimibe
  5. 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。
  6. 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。
  7. 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。
  8. 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。
  9. GC63933 S-Allylmercaptocysteine S-allylmercaptocysteine 是一种从大蒜中提取的有机硫化合物,对各种肺部疾病具有抗炎和抗氧化作用。S-allylmercaptocysteine 通过多种途径发挥抗癌作用,如通过 TGF-β 信号通路诱导癌细胞凋亡 (apoptosis),或通过降低 NF-κb 活性和上调 Nrf2 来达到抗炎和抗氧化的作用。
  10. GC62957 Eriodictyol-7-O-glucoside A flavanone glucoside with diverse biological activities
  11. 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。
  12. 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。
  13. 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。
  14. GC61338 Toralactone Toralactone可从Cassiaobtusifolia中分离得到,通过Nrf2依赖的抗氧化机制介导肝保护。
  15. 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。
  16. GC50242 RA 839 RA 839 是 Keap1 的非共价小分子结合剂,Kd 约为 6 μM,是 Nrf2 信号传导的选择性激活剂。
  17. GC38819 ML334 An inhibitor of the Nrf2-Keap1 protein-protein interaction
  18. 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。
  19. 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。
  20. 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。
  21. 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。
  22. GC44006 Kinsenoside A glycoside with diverse biological activities
  23. 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。
  24. GC40226 Curcumin-d6 An internal standard for the quantification of curcumin
  25. GC34070 Brusatol (NSC 172924) A quassinoid with diverse biological activities
  26. GC34057 TBHQ (tert-Butylhydroquinone) Tert-butylhydroquinone (TBHQ) is an antioxidant compound which is used to prevent lipid peroxidation and shows multiple cytoprotective actions. It is an activator of Nrf2.
  27. 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。

  28. GC33815 4-Hydroxyphenylacetic acid A phenolic acid with anti-inflammatory and anti-steatotic activities
  29. GC33092 Hesperin An isothiocyanate with diverse biological activities
  30. GC32723 CDDO-Im (RTA-403) An activator of Nrf2 signaling
  31. 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.
  32. GC31691 (+)-DHMEQ (+)-DHMEQ 是抗氧化转录因子 Nrf2 的激活剂。
  33. GC31648 4-Octyl Itaconate

    4-Octyl Itaconate 是一种可渗透细胞的衣康酸酯衍生物。

  34. GC31321 KI696 KI696是一种干扰Keap1/NRF2相互作用的高亲和力探针。
  35. GC19254 ML385

    An inhibitor of Nrf2

  36. GC11302 Hinokitiol A tropolone with diverse biological activities
  37. GC13058 NK 252 A Nrf2 activator
  38. GC15457 Pyridoxine A 4-methanol form of vitamin B6
  39. GC14016 Sulforaphane A class I and II HDAC inhibitor with anticancer activity
  40. GC16625 CDDO-TFEA A synthetic triterpenoid with potent anticancer and neuroprotective activity
  41. GC12545 2-HBA An indirect inhibitor of Keap1-Nrf2 interactions
  42. GC12821 Oltipraz A Nrf2 and CAR activator
  43. GC13693 Omaveloxolone (RTA-408) A synthetic triterpenoid that blocks Keap1/Nrf2 signaling
  44. GC17393 Pyridoxine HCl A 4-methanol form of vitamin B6
  45. GC16590 Dimethyl Fumarate An antioxidant with immunological actions
  46. GC15605 Ezetimibe A cholesterol transport inhibitor
  47. GC14787 Curcumin A yellow pigment with diverse biological activities
  48. GC11572 Bardoxolone methyl A synthetic triterpenoid with potent anticancer and antidiabetic activity
  49. GC15371 Bardoxolone An anti-inflammatory compound that activates Nrf2/ARE signaling
  50. GN10629 5,7-dihydroxychromone A flavone decomposition product with diverse biological activities
  51. GN10741 Garcinone D A xanthone with diverse biological activities

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