keap1 nrf2 in 3

Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein-protein interaction inhibitor with a Kd value of 2.5 nM for the KEAP1 protein.

HDAC11-IN-3 (Compound A9) is a selective inhibitor of HDAC11, exhibiting an IC50 value of 4.1 nM. It demonstrates inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines with an IC50 of 10 μM. This compound shows significant anti-AML activity by inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transport proteins transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which collectively increases intracellular iron levels and induces ferroptosis in AML cells. HDAC11-IN-3 can be utilized for AML research either alone or in combination with Cytarabine.

biKEAP1 (compound 3) is an inhibitor that targets the KEAP1 dimer. By binding to cellular KEAP1 dimers, biKEAP1 releases the NRF2 protein that is sequestered by KEAP1, leading to the immediate activation of NRF2. This compound also promotes the nuclear translocation of NRF2 and directly inhibits the transcription of pro-inflammatory cytokines. biKEAP1 has demonstrated the ability to alleviate acute inflammation and reduce inflammatory damage in acute inflammation models.

1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful in protection against bovine mastitis. 3. Farrerol inactivates KEAP-1 or act

Nrf2-IN-3 is a mKEAP1-selective NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2 inhibitory function by repairing the disrupted KEAP1/NRF2 interaction, and selectively sensitizes cisplatin in xenografts of mouse mKEAP1 cancer cells.