| Identification | Back Directory | [Name]
2,6-Phenanthrenedicarbonitrile, 10a-ethynyl-3,4b,7,8,8a,9,10,10a-octahydro-4b,8,8-trimethyl-3,7-dioxo-, (4bR,8aS,10aR)-rel- | [CAS]
936475-62-6 | [Synonyms]
TBE31
TBE-31
TBE 31
2,6-Phenanthrenedicarbonitrile, 10a-ethynyl-3,4b,7,8,8a,9,10,10a-octahydro-4b,8,8-trimethyl-3,7-dioxo-, (4bR,8aS,10aR)-rel- | [Molecular Formula]
C21H18N2O2 | [MOL File]
936475-62-6.mol | [Molecular Weight]
330.38 |
| Hazard Information | Back Directory | [Description]
TBE-31 is a highly potent activator of Nrf2. It also acts as a potent phase 2 cytoprotective pathway inducer and liver carcinogenesis blocker. | [Uses]
TBE 31 is a potent and orally active NQO1 inducer with an Dm value of 1.1 nM. TBE 31 also is a potent Nrf2 activator. TBE 31 reacts with cysteines of Keap1, impairing its ability to target nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) for degradation. TBE 31 shows cytoprotective effects[1][2]. | [References]
[1] Dinkova-Kostova AT, et al. An exceptionally potent inducer of cytoprotective enzymes: elucidation of the structural features that determine inducer potency and reactivity with Keap1. J Biol Chem. 2010 Oct 29;285(44):33747-55. DOI:10.1074/jbc.M110.163485
[2] Kostov RV, et al. Pharmacokinetics and pharmacodynamics of orally administered acetylenic tricyclic bis(cyanoenone), a highly potent Nrf2 activator with a reversible covalent mode of action. Biochem Biophys Res Commun. 2015 Sep 25;465(3):402-7. DOI:10.1016/j.bbrc.2015.08.016 |
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