Nrf2-IN-3

SKU: orb2278364

Description

Nrf2-IN-3 is a selective inhibitor that targets mutant KEAP1, restoring its ability to repress NRF2 signaling. This compound has been shown to enhance cisplatin sensitivity in mouse xenograft models of mKEAP1 cancer, supporting its use in oncology research for investigating the KEAP1/NRF2 pathway in vitro and in vivo.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 6325-13-9
• MW: 442.53
• Purity: 98.07% (May vary between batches)
• Formula: C₂₂H₂₆N₄O₄S
• SMILES: O=C(NN=CC=1C=CC=CC1O)CCCSCCCC(=O)NN=CC=2C=CC=CC2O
• Target: ROS,Nrf2
• Solubility: DMSO:100 mg/mL(225.97 mM)

Bioactivity

• In Vitro:
  Nrf2-IN-3 is a small-molecule NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions. Nrf2-IN-3 substantially sensitizes KEAP1-mutated tumor cells to cisplatin and gefitinib, but does not do so for wild-type KEAP1 cells, and sensitizes KEAP1 G333C-mutated xenograft to cisplatin.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NRF2

Compound Identifiers

PubChem CID

232438