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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.

Products for  KEAP1-Nrf2

  1. Cat.No. 产品名称 Information
  2. GN10654 (+)-Corynoline

    紫蓳灵

     An isoquinoline alkaloid with diverse biological activities
  3. GC31691 (+)-DHMEQ

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-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-羟基-1,7-二苯基-3-庚酮

     (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

    4-羟基苯乙酸

     A phenolic acid with anti-inflammatory and anti-steatotic activities
  7. GC31648 4-Octyl Itaconate

    4-辛基衣康酸

     4-Octyl Itaconate (4-OI) 是一种可渗透细胞的衣康酸酯衍生物。
  8. GN10629 5,7-dihydroxychromone

    5,7-二羟基色酮

     A flavone decomposition product with diverse biological activities
  9. GC16120 AI-3 Nrf2/Keap1 and Keap1/Cul3 interaction inhibitor
  10. GC71544 Antroquinonol Antroquinonol（（+）-Antroquinonol），一种从蘑菇Antrodia camphorata中提取的泛醌衍生物，具有保肝、抗炎和抗癌作用。
  11. GN10415 Astilbin

    落新妇苷

     A flavonoid with diverse biological activities
  12. GC15371 Bardoxolone

    2-氰基-3,12-二氧代齐墩果-1,9-二烯-28-酸,CDDO;RTA 401;RTA401;RTA-401

     An anti-inflammatory compound that activates Nrf2/ARE signaling
  13. GC11572 Bardoxolone methyl

    甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester

     A synthetic triterpenoid with potent anticancer and antidiabetic activity
  14. GC34070 Brusatol (NSC 172924)

    鸦胆子苦醇; NSC 172924

     A quassinoid with diverse biological activities
  15. 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。
  16. GC35629 CDDO-dhTFEA

    RTA dh404

     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。
  17. GC35630 CDDO-EA

    CDDO ethyl amide; TP319; RTA 405

     CDDO-EA 是一种 NF-E2 相关因子 2 /抗氧化反应元件 (Nrf2/ARE) 激活剂。
  18. GC32723 CDDO-Im (RTA-403)

    RTA-403; TP-235; CDDO-Imidazolide

     An activator of Nrf2 signaling
  19. GC14787 Curcumin

    姜黄素; Diferuloylmethane; Natural Yellow 3; Turmeric yellow

     A yellow pigment with diverse biological activities
  20. GC40226 Curcumin-d6

    (1E,4Z,6E)-5-羟基-1,7-二[4-羟基-3-(甲氧基-D3)苯基]-1,4,6-庚三烯-3-酮,Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

     An internal standard for the quantification of curcumin
  21. GN10318 Danshensu

    丹参素

     A salvianolic acid with diverse biological activities
  22. GC34010 Danshensu (Dan shen suan A)

    丹参素; Dan shen suan A; Salvianic acid A

     丹参素是丹参的一种活性成分，通过激活 Nrf2 信号通路显示出广泛的心血管益处。
  23. 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。
  24. GC61419 Dibenzoylmethane

    二苯甲酰甲烷

     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。
  25. GC16590 Dimethyl Fumarate

    富马酸二甲酯

     An antioxidant with immunological actions
  26. GC62936 Dimethyl fumarate D6

    富马酸二甲酯 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。
  27. GC74090 Dimethyl fumarate-d2

    富马酸二甲酯-d2

     Dimethyl fumarate-d2是氘标记的富马酸二甲酯。
  28. GN10531 Dimethylfraxetin

    二甲基白蜡树亭,6,7,8-Trimethoxycoumarin; Fraxetin dimethyl ether

     A coumarin with anti-inflammatory activity
  29. GN10470 Eriodictyol

    圣草酚

     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。
  30. GC62957 Eriodictyol-7-O-glucoside

    圣草酚-7-O-葡糖苷,Eriodictyol 7-O-β-D-glucoside

     A flavanone glucoside with diverse biological activities
  31. GC15605 Ezetimibe

    依泽替米贝; SCH 58235

     A cholesterol transport inhibitor
  32. GC60159 Ezetimibe ketone

    (3R,4S)-1-(4-氟苯基)-3-[3-(4-氟苯基)-3-氧代丙基]-4-(4-羟基苯基)氮杂环丁烷-2-酮,EZM-K

     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。
  33. GC66354 Ezetimibe-d4-1

    SCH 58235-d4-1

     An internal standard for the quantification of ezetimibe
  34. GN10741 Garcinone D

    伽升沃 D

     A xanthone with diverse biological activities
  35. GN10038 Ginsenoside Rh3

    人参皂苷 Rh3

     Ginsenoside Rh3 是 Ginsenoside Rg5 的细菌代谢产物。
  36. GC33092 Hesperin

    6-MSITC

     An isothiocyanate with diverse biological activities
  37. GC11302 Hinokitiol

    桧木醇; β-Thujaplicin

     A tropolone with diverse biological activities
  38. GC71232 I-152 I-152是含有n -乙酰半胱氨酸(NAC)和半胱胺(MEA)的缀合物。
  39. 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。
  40. 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。
  41. GC31321 KI696 KI696是一种干扰Keap1/NRF2相互作用的高亲和力探针。
  42. 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。
  43. GC44006 Kinsenoside

    金线莲苷

     A glycoside with diverse biological activities
  44. GN10491 Mangiferin

    芒果苷

     A xanthone glucoside with diverse biological activities
  45. GC31783 Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester)

    3,4-二羟基苯甲酸甲酯,Protocatechuic acid methyl ester; Methyl protocatechuate

     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.
  46. GC70520 MIND4-17 MIND4-17是一种强效的NRF2激活剂，共价修饰Keap1的C151残基。
  47. GC38819 ML334

    LH601A

     ML334是一种有效的NRF2细胞渗透性激活剂。
  48. GC19254 ML385 ML385是一种特定的核因子红细胞2相关因子2（NRF2）抑制剂。
  49. GC13058 NK 252 A Nrf2 activator
  50. 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。
  51. GC70868 Nrf2 activator-3 Nrf2 activator-3是一种有效的Nrf2激活剂。

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