Bardoxolone

Bardoxolone (CDDO; RTA 401) is a Nrf2 activator. Bardoxolone shows anti-SARS-CoV-2 3CLpro with IC50 of 27.99 μM. Bardoxolone activates the Nrf2 pathway and inhibits the NF-κB pathway. Bardoxolone can induce cells differentiation, apoptosis and shows antiproliferative activity against cancer cells. Bardoxolone can increase ROS and decrease intracellular GSH levels. Bardoxolone inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis. Bardoxolone can be used for the research of cancer, inflammation and infection, such as SARS-CoV infection and glioblastoma^[1][2][3]. IC50 & Target:Nrf-2^[1] In Vitro:Bardoxolone (30 min) reversibly covalently inhibits SARS-CoV-2 3CLpro with an IC₅₀ of 27.99 ± 2.34 μM and a dissociation constant of 25.90 μM^[1].
Bardoxolone (48 h) inhibits SARS-CoV-2 replication in Vero and Calu-3 cells with EC₅₀ values of 0.43 and 0.42 μM and selective index of 56.6 and 28.2^[1].
Bardoxolone (10-100 nM) induces adipocyte differentiation in 3T3-L1 preadipocytes^[2].
Bardoxolone induces differentiation in acute promyelocytic leukemia cell lines (HL-60, NB4, MR2) and primary AML blasts via PPAR-γ-dependent mechanisms, including enhancement of ATRA-induced effects^[2].
Bardoxolone induces differentiation in osteosarcoma cells via a PPAR-γ-independent mechanism mediated by caspase-8 activity^[2].
Bardoxolone (1-10 μM) exerts antiproliferative and proapoptotic effects in lymphoma and colon cancer cells via inhibition of Lonp1 activity^[2].
Bardoxolone (1-10 μM) induces apoptosis in glioblastoma (U87MG, U251MG) and neuroblastoma (SK-N-MC) cell lines^[2].
Bardoxolone (1-10 μM) induces intrinsic pathway apoptosis in U-937 leukemia cells with increased ROS and decreased intracellular GSH^[2].
Bardoxolone (0.08-10 μM; pre-incubation + 12-16 h) inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis in HT-29 cells with an EC₅₀ of 1.30 ± 0.38 μM^[3].