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.

Nrf2 activator-21 is a compound that serves as an Nrf2 activator with both antioxidant and neuroprotective properties. It binds to the Keap1Kelch domain, disrupting the Keap1-Nrf2 interaction and activating antioxidant defense mechanisms. Nrf2 activator-21 decreases apoptosis of hippocampal neurons and reduces caspase-3 activity. It targets cerebral ischemia/reperfusion injury (CIRI) by activating the Nrf2 pathway. The compound improves neurological function, alleviates anxiety-like behavior induced by bilateral carotid artery occlusion (2VO) in rats, and enhances memory. Nrf2 activator-21 is applicable in studies of cerebral ischemia/reperfusion injury.

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.

Farrerol (Standard) is a reference standard for research and analysis in studies involving Farrerol. 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 activates the Akt, p38 and ERK to facilitate the release of Nrf2 from Keap1 and subsequent reduces the intracellular production of reactive oxygen species via the induction of HO-1 expression. 4. Farrerol has protective effects against H2O2-induced apoptosis in EA.hy926 cells, and suggests that Farrerol is a potential candidate for the intervention of endothelial-injury-associated cardiovascular diseases.