GPX4-AUTAC
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne , a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394) ).
Product Specifications
CAS Number
3060458-90-1
UNSPSC
12352005
Target
AUTACs; Autophagy; Ferroptosis; Glutathione Peroxidase
Related Pathways
Apoptosis; Autophagy; Metabolic Enzyme/Protease; PROTAC
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Cancer
Smiles
O=C(C(N(C1=CC(Cl)=C(OCC(N=N2)=CN2CCOCCOCCOCCNC([C@H](CSC3=NC4=C(N3CC5=CC=C(C=C5)F)N=C(NC4=O)N)NC(C)=O)=O)C=C1)C(CCl)=O)C6=CC=CS6)NCCC7=CC=CC=C7
Molecular Formula
C50H55Cl2FN12O9S2
Molecular Weight
1122.08
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
GPX4
Frequently Asked Questions
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