PROTAC GPX4 degrader-4

PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM) . PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively) . PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193) ; blue: E3 ligase ligand (HY-1035960) ; black: linker (HY-W013907) ; E3 ligase ligand + linker (HY-174087) ) [1].

Product Specifications

CAS Number

[3071165-43-7]

UNSPSC

12352005

Target

Ferroptosis; Glutathione Peroxidase; PROTACs; ROS Kinase

Related Pathways

Apoptosis; Metabolic Enzyme/Protease; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

C[C@@H]1[C@@]2([H])[C@]34[C@](O[C@](OO3)(CC[C@@]4([H])[C@@H](CC2)C)C)([H])O[C@H]1OC(CCC(OCCCCCCCCCCCOC5=C6C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)=CC=C5)=O)=O

Molecular Formula

C43H58N2O13

Molecular Weight

810.93

References & Citations

[1]Yang X, et al. Discovery of Artesunate (ARS) PROTACs as GPX4 protein degraders for the treatment of bladder cancer. Eur J Med Chem. 2025 Sep 5;293:117710.