TBE-31

TBE-31 is a highly potent, reversible covalent small molecule activator of the Nrf2 (nuclear factor erythroid 2-related factor 2) pathway. It belongs to the acetylenic tricyclic bis(cyano enone) class. TBE-31 primarily functions by binding to the Cys151 residue of Keap1 (Kelch-like ECH-associated protein 1), the negative regulator of Nrf2, thereby preventing Nrf2 degradation and allowing it to orchestrate the expression of cytoprotective and antioxidant genes. Beyond Nrf2 activation, TBE-31 has been shown to interact with the cytoskeleton by binding to Cys374 of actin and interfering with microtubule dynamics, which contributes to its ability to inhibit cell migration. It has demonstrated efficacy in preclinical models for a variety of conditions, including nonalcoholic steatohepatitis (NASH), liver fibrosis, obesity, and UV-induced skin damage.

Other names

acetylenic tricyclic bis(cyano enone)(±)-(4bS,8aR,10aS)-10a-ethynyl-4b,8,8-trimethyl-3,7-dioxo-3,4b,7,8,8a,9,10,10a-octahydrophenanthrene-2,6-dicarbonitriletricyclic bis(cyano enone)