3-Methyltoxoflavin 是蛋白质二硫键异构酶抑制剂(IC50:170 nM)。
产品描述
3-methyltoxoflavin is an effective inhibitor of protein disulfide isomerase (PDI) and its IC50 value is 170 nM.
体外活性
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. 3-Methyltoxoflavin emerges as the most cytotoxic inhibitor of PDI from the screen. 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.
Cas No.
32502-62-8
分子式
C8H9N5O2
分子量
207.193
别名
3-methyl toxoflavin;3-Methyltoxoflavin
储存和溶解度
DMSO:150 mg/mL (723.97 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years