3-Methyltoxoflavin

SKU: orb1301779

Description

3-Methyltoxoflavin is a potent small molecule inhibitor of protein disulfide isomerase (PDI) with an IC50 of 170 nM. This compound is a valuable research tool for studying PDI function in protein folding and thrombosis models, applicable in both biochemical and cellular assays.

Key Properties

• CAS Number: 32502-62-8
• MW: 207.19
• Purity: 99.84% (May vary between batches)
• Formula: C₈H₉N₅O₂
• SMILES: Cc1nn(C)c2nc(=O)n(C)c(=O)c2n1
• Target: Others
• Solubility: DMSO:150 mg/mL (723.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (24.13 mM)

Bioactivity

• Target IC50:
  PDI:170 nM
• In Vitro:
  3-Methyltoxoflavin is an effective inhibitor of Protein disulfide isomerase (PDI), exhibiting significant potency with an IC50 value of 170 nM, and demonstrating marked toxicity across various human glioblastoma cell lines. It stands out as the most potent PDI inhibitor identified in screening efforts. Research involving Bromouridine labeling and sequencing (Bru-seq) has shown that 3-Methyltoxoflavin activates the Nrf2 antioxidant response, triggers ER stress response, and promotes autophagy. It achieves this by increasing the transcription and protein levels of heme oxygenase 1 and SLC7A11, while simultaneously downregulating expression of PDI target genes, such as TXNIP and EGR1. Notably, the cell death induced by 3-Methyltoxoflavin does not occur through traditional pathways like apoptosis or necrosis, but rather through a combination of autophagy and ferroptosis.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

protein disulfide isomerase (PDI), Inhibitor, inhibit, 3-methyl toxoflavin, 3Methyltoxoflavin, 3-Methyltoxoflavin, 3 Methyltoxoflavin

Compound Identifiers

PubChem CID

460747