| Description | 3-Methyltoxoflavin (3-methyl toxoflavin) is an effective inhibitor of protein disulfide isomerase (PDI) and its IC50 value is 170 nM. |
| In vitro | 3-Methyltoxoflavin是一种强效的蛋白质二硫键异构酶(PDI)抑制剂，IC50为170 nM。在一系列人类胶质母细胞瘤细胞线中表现出毒性。3-Methyltoxoflavin被筛选为最具细胞性毒性的PDI抑制剂。溴尿苷标记和测序(Bru-seq)新生RNA揭示3-Methyltoxoflavin诱导Nrf2抗氧化应答、内质网应激反应和自噬。具体而言，3-Methyltoxoflavin上调血红素加氧酶1和SLC7A11的转录及蛋白表达，并抑制PDI靶基因如TXNIP和EGR1。有趣的是，3-Methyltoxoflavin引起的细胞死亡不通过凋亡或坏死进行，而是通过自噬和铁死亡的混合方式。 |
| Target activity | PDI:170 nM |
| Synonyms | 3-methyl toxoflavin |
| molecular weight | 207.19 |
| Molecular formula | C8H9N5O2 |
| CAS | 32502-62-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 150 mg/mL (723.97 mM) |
| References | 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. |