Keap1-Nrf2 is the major regulator of cytoprotective responses to oxidative and electrophilic stress. Kelch-like ECH-associated protein 1 is a protein that in humans is encoded by the Keap1 gene. Keap1 has been shown to interact with Nrf2, a master regulator of the antioxidant response, which is important for the amelioration of oxidative stress. Under quiescent conditions, Nrf2 is anchored in the cytoplasm through binding to Keap1, which, in turn, facilitates the ubiquitination and subsequent proteolysis of Nrf2. Such sequestration and further degradation of Nrf2 in the cytoplasm are mechanisms for the repressive effects of Keap1 on Nrf2. because Nrf2 activation leads to a coordinated antioxidant and anti-inflammatory response, and Keap1 represses Nrf2 activation, Keap1 has become a very attractive drug target.


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NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
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Nrf2 activator-6

Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4)[1].

  • CAS Number: 2728780-74-1
  • MF: C31H37ClFN5O5
  • MW: 614.11
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AEM1

NRF2 inhibitor AEM1 is a specific small molecule inhibitor of Nrf2 transcriptional activity in cancer cells, shows no activity against a panel of >100 kinases (including isoforms of PI3K, AKT, and PKC); broadly decreases the expression of Nrf2 controlled genes (HMOX1, GPX2), sensitizes A549 cells to various chemotherapeutic agents, and inhibits the growth of A549 cells in vitro and in vivo.

  • CAS Number: 1030123-90-0
  • MF: C20H14FN3O2S
  • MW: 379.408
  • Catalog: Keap1-Nrf2
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 582.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 305.9±30.1 °C

Bardoxolone

Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.

  • CAS Number: 218600-44-3
  • MF: C31H41NO4
  • MW: 491.661
  • Catalog: Keap1-Nrf2
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 632.9±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 336.6±31.5 °C

CDDO-EA

CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.

  • CAS Number: 932730-51-3
  • MF: C33H46N2O3
  • MW: 518.738
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A