2. PROTAC Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Molecular Glues Glutathione Peroxidase Ferroptosis Reactive Oxygen Species (ROS)
  4. GPX4 degrader-2

GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer.

For research use only. We do not sell to patients.

GPX4 degrader-2

GPX4 degrader-2 Chemical Structure

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GPX4 degrader-2 Related Antibodies

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Description

GPX4 degrader-2 is a GPX4 molecular glue degrader and ferroptosis inducer. GPX4 degrader-2 suppresses GPX4 enzyme activity, promotes ubiquitination-dependent proteasomal degradation of GPX4 protein. GPX4 degrader-2 indues ferroptosis, increases lipid ROS and MDA levels, suppresses glutathione levels in cancer cells. GPX4 degrader-2 inhibits cancer cells proliferation and colony formation. GPX4 degrader-2 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

GPX4

 

In Vitro

GPX4 degrader-2 (Compound W25) (24-72 h) potently inhibits HCT-116 colorectal cancer cell viability with time-dependent efficacy, achieving IC50 values of 4.17, 2.49 and 2.24 μM after 24. 48 and 72 h treatment[1].
GPX4 degrader-2 (2.5-10 μM; 6 h) dose-dependently suppresses long-term colony formation of HCT-116 colorectal cancer cells and inhibits DNA synthesis[1].
GPX4 degrader-2 (2.5-10 μM; 6-24 h) dose- and time-dependently accumulates lipid ROS in HCT-116 colorectal cancer cells[1].
GPX4 degrader-2 (2.5-10 μM; 24 h) dose-dependently depletes intracellular GSH levels and increases intracellular MDA levels in HCT-116 colorectal cancer cells[1].
GPX4 degrader-2 (2.5-10 μM; 6-24 h) dose-dependently downregulates GPX4 protein expression in HCT-116 colorectal cancer cells by promoting ubiquitin-proteasomal degradation[1].
GPX4 degrader-2 (10 μM; 24 h) promotes ubiquitination of GPX4 protein in HCT-116 colorectal cancer cells[1].
GPX4 degrader-2 (50-100 μM; 2 h) directly binds to GPX4 protein, protecting it from pronase E digestion in HCT-116 colorectal cancer cell lysates[1].
GPX4 degrader-2 inhibits the enzymatic activity of human recombinant GPX4[1].

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

GPX4 degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT-116 colorectal cancer cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 6, 12, 24 h
Result: Reduced GPX4 protein levels.
Had its GPX4-inhibitory effect reversed by MG132 treatment.
Molecular Weight

568.01

Formula

C30H30ClNO8
SMILES

O=C(OC1=CC=C(C[C@H]2C(OCC2CC3=CC=C(OC)C(OC)=C3)=O)C=C1OC)C4=CC=C(NC(CCl)=O)C=C4
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GPX4 degrader-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GPX4 degrader-2Molecular GluesGlutathione PeroxidaseFerroptosisReactive Oxygen Species (ROS)glutathioneubiquitin-proteasomal degradationhuman liver microsomesmalondialdehydeGPX4lipid reactive oxygen speciesferroptosiscolorectal cancer cellsHCT-116 colorectal cancer cellubiquitination-dependent proteasomal degradationInhibitorinhibitorinhibit

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GPX4 degrader-2
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