Keap1-Nrf2 Degrader

Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC₅₀ of 0.1-1 μM in huH1 cells. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC₅₀ values of 100 nM and 40 nM, respectively. Nrf2 degrader 1 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer.

Angelic acid is a ferroptosis inducer, targeting NRF2 degradation. Angelic acid binds to NRF2 protein and promotes NRF2 degradation via ubiquitination-proteasome pathway, relieves the inhibitory effect of NRF2 on oxidative stress and lipid peroxidation. Then, Angelic acid induces ferroptosis in tumor cells. Angelic acid can enhance the accumulation of intracellular reactive oxygen species (ROS), upregulate ferroptosis-related markers CHAC1 and PTGS2, and synergize with ferroptosis inducers to enhance anti-tumor effects. Angelic acid also has the activity of scavenging UVA-induced ROS in vitro, inhibiting skin fibroblast senescence and extracellular matrix degradation. Angelic Acid helps wound healing with sedative activity.

Flumethasone (Flumetasone) is an orally active, high selective and potent glucocorticoid receptor (GR) agonist. Flumethasone activates GR to inhibit nuclear factor kappa B (NF-κB)-mediated pro-inflammatory cytokine production (TNF-α, IL-1β) and promotes anti-inflammatory gene expression (IL-10), while also regulating metabolic enzyme activity (tyrosine aminotransferase induction). Flumethasone is promising for research of inflammatory diseases, cancer, and endocrine regulation.

VVD 065 is an orally active KEAP1-dependent NRF2 molecular glue degrader with a KEAP1 K_D of 65 nM. VVD 065 covalently engages KEAP1 at Cys151, allosterically stabilizes KEAP1-CUL3 complex formation and enhances NRF2 polyubiquitination and proteasomal degradation. VVD 065 can be used for the research of esophageal squamous cell carcinoma, lung cancer, head-and-neck cancer, uterine cancers.

Angelic acid (Standard)) is the analytical standard of Angelic acid (HY-N6929). This product is intended for research and analytical applications. Angelic acid is a ferroptosis inducer, targeting NRF2 degradation. Angelic acid binds to NRF2 protein and promotes NRF2 degradation via ubiquitination-proteasome pathway, relieves the inhibitory effect of NRF2 on oxidative stress and lipid peroxidation. Then, Angelic acid induces ferroptosis in tumor cells. Angelic acid can enhance the accumulation of intracellular reactive oxygen species (ROS), upregulate ferroptosis-related markers CHAC1 and PTGS2, and synergize with ferroptosis inducers to enhance anti-tumor effects. Angelic acid also has the activity of scavenging UVA-induced ROS in vitro, inhibiting skin fibroblast senescence and extracellular matrix degradation. Angelic Acid helps wound healing with sedative activity.

PROTAC Nrf2 degrader-1 is a PROTAC degrader targeting Nrf2, with IC₅₀ values of 10 nM and 3 nM in A549 cells and LK-2 cells, respectively. PROTAC Nrf2 degrader-1 can be used in cancer research.