RGNCY-0084 (35G8 PDI inhibitor)

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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.

Systematic Name: 1,3,6-trimethylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
Formula: C8H9N5O2
Mol Wt:  207.08
PMID:  29235250

Tags: autophagy, small molecule, glioma, Glioblastoma, RGNCY-0084, 35G8, PDI, Nrf2, SLC7A11, TXNIP, ferroptosis