21105-15-7
Chemical Structure
Obtusaquinone
- CAS No.: 21105-15-7
- Formula:C16H14O3
- Molecular Weight:254.28
InChIKey: LUZUAYAKZLCOCQ-BHHNFLQBSA-N
SMILES: COC(/C1=C/C=C/C2=CC=CC=C2)=CC(C(O)=C1)=O
Biological Activity: Obtusaquinone is a blood-brain barrier-permeable Keap1 inhibitor with anticancer activity. Obtusaquinone covalently binds to cysteine residues of Keap1, promotes its ubiquitination and proteasomal degradation, and activates the Nrf2 pathway. Obtusaquinone induces endoplasmic reticulum stress and DNA damage through abnormal accumulation of ROS, and triggers apoptosis of cancer cells. Obtusaquinone prolongs survival in orthotopic xenograft models of pediatric high-grade glioma, and exhibits antitumor activity in glioblastoma and breast cancer models. Obtusaquinone can be used in studies related to glioma and breast cancer[1][2].
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Obtusaquinone | Obtusaquinone is a blood-brain barrier-permeable Keap1 inhibitor with anticancer activity. Obtusaquinone covalently binds to cysteine residues of Keap1, promotes its ubiquitination and proteasomal degradation, and activates the Nrf2 pathway. Obtusaquinone induces endoplasmic reticulum stress and DNA damage through abnormal accumulation of ROS, and triggers apoptosis of cancer cells. Obtusaquinone prolongs survival in orthotopic xenograft models of pediatric high-grade glioma, and exhibits antitumor activity in glioblastoma and breast cancer models. Obtusaquinone can be used in studies related to glioma and breast cancer. | |||||||||||||||||||||
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- [1]. Teng J, et al. The natural compound obtusaquinone targets pediatric high-grade gliomas through ROS-mediated ER stress. Neuro-oncology advances. 2020;2(1):vdaa106. [Content Brief]
- [2]. Badr CE, et al. Obtusaquinone: A Cysteine-Modifying Compound That Targets Keap1 for Degradation. ACS chemical biology. 2020 Jun 19;15(6):1445-1454. [Content Brief]
Keywords
