35G8 PDI inhibitor RGNCY-0084
Per 10 mg
35G8 is a novel nanomolar PDI (protein disulfide isomerase) inibitor that is toxic in a panel of human glioblastoma cell lines, PDI is overexpressed in glioblastoma and folds nascent protein responsible for the progression and spread of this brain cancer. 35G8 induces nuclear factor-like 2 (Nrf2) anti-oxidant response, endoplasmic reticulum stress response and autophagy. 35G8 upregulates heme oxygenase 1 and solute carrier family 7 member 11 (SLC7A11) transcription and protein expression and repressed PDI target genes including thioredoxin-interacting protein 1 (TXNIP) and early growth respoinse 1 (EGFR1). 35G8 indices cell death via autophagy and ferroptosis rather than apoptosis or necrosis. 35G8 can be used as chemical probe to validate PDI as a target for brain tumor therapy. Insulin turbidity assay IC50 = 170+10nM.
Kyani A et al. Discovery and Mechanistic Elucidation of a Class of Protein Disulfide Isomerase Inhibitors for the Treatment of Glioblastoma. ChemMedChem 2018, 13, 164 – 177.
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