3-Methyltoxoflavin |
| Katalog-Nr.GC33060 |
3-Methyltoxoflavin ist ein potenter Hemmer der Proteindisulfidisomerase (PDI) mit einem IC50-Wert von 170 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 32502-62-8
Sample solution is provided at 25 µL, 10mM.
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3-Methyltoxoflavin is a potent Protein disulfide isomerase (PDI) inhibitor, with an IC50 of 170 nM.
3-Methyltoxoflavin is a potent Protein disulfide isomerase (PDI) inhibitor, with an IC50 of 170 nM. 3-Methyltoxoflavin is toxic in a panel of human glioblastoma cell lines. From the screen, 3-Methyltoxoflavin emerges as the most cytotoxic inhibitor of PDI. Bromouridine labeling and sequencing (Bru-seq) of nascent RNA reveals that 3-Methyltoxoflavin induces Nrf2 antioxidant response, ER stress response, and autophagy. Specifically, 3-Methyltoxoflavin upregulates heme oxygenase 1 and SLC7A11 transcription and protein expression and represses PDI target genes such as TXNIP and EGR1. Interestingly, 3-Methyltoxoflavin-induced cell death does not proceed via apoptosis or necrosis, but by a mixture of autophagy and ferroptosis[1].
[1]. Kyani A, et al. Discovery and Mechanistic Elucidation of a Class of Protein Disulfide Isomerase Inhibitors for the Treatment of Glioblastoma. ChemMedChem. 2018 Jan 22;13(2):164-177.
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