GPX4-IN-20 

GPX4-IN-20, a Arctigenin (HY-N0035) derived, is a GPX4& molecular gluedegrader. GPX4-IN-20 induces ferroptosis by increasing lipid ROS levels and suppressing GSH levels. GPX4-IN-20 reduces the protein expression and enzyme activity of GPX4 in a dose-dependent manner without affecting other ferroptosis-related proteins. GPX4-IN-20 induces ubiquitination-dependent proteasomal degradation of GPX4. GPX4-IN-20 also increases the level of malondialdehyde (MDA) in HCT-116 cells. GPX4-IN-20 can be used for the research of colorectal cancer^[1].

GPX4-IN-20 (compound W25) (2.5-10 μM; 24-72 h) shows cytotoxic activity on HCT-116 cells^[1].
GPX4-IN-20 (2.5-10 μM; 24 hours; HCT-116 cells) inhibits GPX4 protein expression and activity, promoting ubiquitination-dependent proteasomal degradation. GPX4-IN-20 has no significant effect on other key regulatory factors of ferroptosis, such as ferroptosis suppressor protein 1 (FSP1), ferritin heavy chain 1 (FTH1), nuclear receptor coactivator 4 (NCOA4), and solute carrier family 7 member 11 (SLC7A11)^[1].
GPX4-IN-20 (2.5-10 μM; 24 hours; HCT-116 cells) does not affect GPX4 mRNA levels^[1].
GPX4-IN-20 (0, 2.5, 5, 10 μM; 6 h) inhibits the clone formation of HCT-116 cells in a dose-dependent manner^[1].
GPX4-IN-20 (24 h) inhibits the cell growth of HT-29 with an IC₅₀ of 4.60 μM^[1].
GPX4-IN-20 (0, 2.5, 5, 10 μM; 6, 12, 24 hours; HCT-116 cells) significantly increases the lipid ROS levels in HCT-116 cells with a dose- and time-dependent manner. GPX4-IN-20 significantly decreases GPX4 levels. After treatment with GPX4-IN-20, intracellular MDA content is increased in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

568.01

C₃₀H₃₀ClNO₈

ClCC(NC(C=C1)=CC=C1C(OC(C(OC)=C2)=CC=C2C[C@@H](C(OC3)=O)[C@H]3CC4=CC(OC)=C(OC)C=C4)=O)=O

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• [1]. Wang YX, et al. Design, synthesis, and biological evaluation of arctigenin derivatives as novel GPX4 inhibitors in colorectal cancer cells. Eur J Med Chem. 2025;300:118181.  [Content Brief]