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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.

Products for  KEAP1-Nrf2

  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

    SCH 58235-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-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。
  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

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

    A flavanone glucoside with diverse biological activities
  11. 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。
  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

    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。
  14. GC61338 Toralactone

    决明内酯

    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

    (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。
  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

    LH601A

    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 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。
  21. 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。
  22. GC44006 Kinsenoside

    金线莲苷

    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

    (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
  25. GC34070 Brusatol (NSC 172924)

    鸦胆子苦醇; NSC 172924

    A quassinoid with diverse biological activities
  26. GC34057 TBHQ (tert-Butylhydroquinone)

    特丁基对苯二酚; tert-Butylhydroquinone

    TBHQ(tert-Butylhydroquinone)是Nrf2 激活剂,并有抗炎、抗氧化、抗凋亡和神经保护作用。

  27. GC34010 Danshensu (Dan shen suan A)

    丹参素; Dan shen suan A; Salvianic acid 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

    4-羟基苯乙酸

    A phenolic acid with anti-inflammatory and anti-steatotic activities
  29. GC33092 Hesperin

    6-MSITC

    An isothiocyanate with diverse biological activities
  30. GC32723 CDDO-Im (RTA-403)

    RTA-403; TP-235; CDDO-Imidazolide

    An activator of Nrf2 signaling
  31. 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.
  32. GC31691 (+)-DHMEQ

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ

    (+)-DHMEQ 是抗氧化转录因子 Nrf2 的激活剂。
  33. GC31648 4-Octyl Itaconate

    4-辛基衣康酸

    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

    桧木醇; β-Thujaplicin

    A tropolone with diverse biological activities
  37. GC13058 NK 252 A Nrf2 activator
  38. GC15457 Pyridoxine

    吡哆醇; Pyridoxol

    A 4-methanol form of vitamin B6
  39. GC14016 Sulforaphane

    萝卜硫素

    A class I and II HDAC inhibitor with anticancer activity
  40. GC16625 CDDO-TFEA

    CDDO-Trifluoethyl Amide,RTA 404,TP-500

    A synthetic triterpenoid with potent anticancer and neuroprotective activity
  41. GC12545 2-HBA

    Bis(2-hydroxybenzylidene)acetone

    An indirect inhibitor of Keap1-Nrf2 interactions
  42. GC12821 Oltipraz

    奥替普拉; RP 35972; NSC 347901

    A Nrf2 and CAR activator
  43. GC13693 Omaveloxolone (RTA-408)

    RTA 408

    A synthetic triterpenoid that blocks Keap1/Nrf2 signaling
  44. GC17393 Pyridoxine HCl

    吡哆醇盐酸盐; Pyridoxol hydrochloride; Vitamin B6 hydrochloride

    A 4-methanol form of vitamin B6
  45. GC16590 Dimethyl Fumarate

    富马酸二甲酯

    An antioxidant with immunological actions
  46. GC15605 Ezetimibe

    依泽替米贝; SCH 58235

    A cholesterol transport inhibitor
  47. GC14787 Curcumin

    姜黄素; Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    A yellow pigment with diverse biological activities
  48. 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
  49. 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
  50. GN10629 5,7-dihydroxychromone

    5,7-二羟基色酮

    A flavone decomposition product with diverse biological activities
  51. GN10741 Garcinone D

    伽升沃 D

    A xanthone with diverse biological activities

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