3-Methyltoxoflavin是蛋白质二硫键异构酶(PDI)的有效抑制剂，其IC50值为170nM。
CAS：32502-62-8
分子式：C8H9N5O2
分子量：207.19
纯度：98%
存储：Store at -20°C

Background:

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.