Background
CDDO-Me (bardoxolone methyl) is a synthetic triterpenoid that induces apoptosis and differentiation in cancer cells, and exhibits strong antiproliferative and antiangiogenic activities (1). CDDO-Me activates nuclear factor-like 2 (NRF2) transcriptional activator, which regulates oxidative stress response gene expression through binding of antioxidant response element (ARE) promoter gene regions. CDDO-Me interacts with the NRF2 inhibitor INrf2 (also called KEAP1), resulting in the release of NRF2 from the proteasome pathway and translocation of NRF2 into the nucleus (2). Additionally, CDDO-Me binds IKKβ to block the targeting of NF-κB p65 to the nucleus and inhibits NF-κB activation and downstream pro-inflammatory signaling pathways (3). CDDO-Me has been studied as an anticancer and anti-inflammatory drug, with potential to treat patients with chronic kidney disease associated with diabetes (4). Low doses of CDDO-Me may exert therapeutic effects on cardiac function in models of chronic heart failure (5).
- Borella, R. et al. (2019) Molecules 24, 4097. doi: 10.3390/molecules24224097.
- Liby, K.T. and Sporn, M.B. (2012) Pharmacol Rev 64, 972-1003.
- Wang, Y.Y. et al. (2014) Drug Des Devel Ther 8, 2075-88.
- Kanda, H. and Yamawaki, K. (2020) Clin Exp Nephrol 24, 857-864.
- Tian, C. et al. (2019) J Pharmacol Exp Ther 371, 642-651.
Molecular Formula
C32H43NO4
Molecular Weight
505.7 g/mol
Purity
>98%
CAS
218600-53-4
Solubility
Soluble in DMSO at 25 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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