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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. Product Name Information
  2. GC31691 (+)-DHMEQ (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ Chemical Structure
  3. GC65610 (R)-5-Hydroxy-1,7-diphenyl-3-heptanone (R)-5-Hydroxy-1,7-diphenyl-3-heptanone is a diarylheptanoid that can be found in Alpinia officinarum. (R)-5-Hydroxy-1,7-diphenyl-3-heptanone Chemical Structure
  4. GC15355 2-Trifluoromethyl-2'-methoxychalcone Nrf2 activator 2-Trifluoromethyl-2'-methoxychalcone Chemical Structure
  5. GC33815 4-Hydroxyphenylacetic acid A phenolic acid with anti-inflammatory activity 4-Hydroxyphenylacetic acid Chemical Structure
  6. GC31648 4-Octyl Itaconate

    4-Octyl Itaconate?(4-OI) is a cell-permeable itaconate derivative. Itaconate and 4-Octyl Itaconate?had similar thiol reactivity, making 4-Octyl Itaconate?a suitable itaconate surrogate to study its biological function.

     4-Octyl Itaconate Chemical Structure
  7. GC16120 AI-3 Nrf2/Keap1 and Keap1/Cul3 interaction inhibitor AI-3 Chemical Structure
  8. GC34070 Brusatol (NSC 172924) Brusatol (NSC 172924) (NSC172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol (NSC 172924) enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol (NSC 172924) can be developed into an adjuvant chemotherapeutic agent. Brusatol (NSC 172924) increases cellular apoptosis. Brusatol (NSC 172924) Chemical Structure
  9. GC35629 CDDO-dhTFEA CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA Chemical Structure
  10. GC35630 CDDO-EA CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator. CDDO-EA Chemical Structure
  11. GC32723 CDDO-Im (RTA-403) CDDO-Im (RTA-403) (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ. CDDO-Im (RTA-403) Chemical Structure
  12. GC40226 Curcumin-d6 Curcumin-d6 is intended for use as an internal standard for the quantification of curcumin by GC- or LC-MS. Curcumin-d6 Chemical Structure
  13. GC64971 DDO-7263 DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 Chemical Structure
  14. GC16590 Dimethyl Fumarate nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator Dimethyl Fumarate Chemical Structure
  15. GC15605 Ezetimibe Cholesterol transport inhibitor Ezetimibe Chemical Structure
  16. GC66354 Ezetimibe-d4-1 Ezetimibe-d4 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe-d4-1 Chemical Structure
  17. GC33092 Hesperin An isothiocyanate with diverse biological activities Hesperin Chemical Structure
  18. GC11302 Hinokitiol A tropolone with diverse biological activities Hinokitiol Chemical Structure
  19. GC66004 K67 K67 specifically inhibits the interaction between Keap1 and S349-phosphorylated p62. K67 prevents p-p62 from blocking the binding of Keap1 and Nrf2. K67 effectively inhibits the proliferation of HCC cultures with high cellular S351-phosphorylated p62 by restoring the ubiquitination and degradation of Nrf2 driven by Keap1. K67 Chemical Structure
  20. GC36390 Keap1-Nrf2-IN-1 Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 Chemical Structure
  21. GC31321 KI696 KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 Chemical Structure
  22. GC34642 KI696 isomer KI696 isomer is the less active isomer of KI696. KI696 isomer Chemical Structure
  23. GC31783 Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester) Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester) (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester) Chemical Structure
  24. GC38819 ML334 An inhibitor of the Nrf2-Keap1 protein-protein interaction ML334 Chemical Structure
  25. GC19254 ML385

    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor.

     ML385 Chemical Structure
  26. GC13058 NK 252 Nrf2 activator NK 252 Chemical Structure
  27. GC69590 Nrf2 activator-2

    Nrf2 activator-2 (compound O15) is a derivative of sulforaphane, an effective Nrf2 activator with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thereby showing an activating effect on Nrf2. Nrf2 activator-2 significantly reduces the level of ubiquitinated Nrf2 in cells.

     Nrf2 activator-2 Chemical Structure
  28. GC66054 Nrf2 activator-4 Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 μM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model. Nrf2 activator-4 Chemical Structure
  29. GC36773 Nrf2-IN-1 Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML). Nrf2-IN-1 Chemical Structure
  30. GC12821 Oltipraz Nrf2 activator;An antischistosomal agent Oltipraz Chemical Structure
  31. GC13693 Omaveloxolone (RTA-408) Omaveloxolone (RTA-408) (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone (RTA-408) Chemical Structure
  32. GC15457 Pyridoxine A 4-methanol form of vitamin B6 Pyridoxine Chemical Structure
  33. GC17393 Pyridoxine HCl Pyridoxine HCl (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine HCl Chemical Structure
  34. GC63933 S-Allylmercaptocysteine S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-Allylmercaptocysteine Chemical Structure
  35. GC14352 TAT 14 Nrf2 activator TAT 14 Chemical Structure
  36. GC34057 TBHQ (tert-Butylhydroquinone) TBHQ (tert-Butylhydroquinone) (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma. TBHQ (tert-Butylhydroquinone) Chemical Structure

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