2. Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Glutathione Peroxidase Ferroptosis Reactive Oxygen Species (ROS)
  4. GPX4-IN-24

GPX4-IN-24 is an orally active glutathione peroxidase 4 (GPX4) inhibitor with a human IC50 of 10.90 μM, human Kd of 10.04 μM. GPX4-IN-24 suppresses GPX4 enzymatic activity, disrupts redox homeostasis, drives lipid peroxidation, promotes lipid peroxidation, and induces ferroptosis. GPX4-IN-24 can be used for the research of triple-negative breast cancer.

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

GPX4-IN-24

GPX4-IN-24 Chemical Structure

CAS No. : 2834106-56-6

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GPX4-IN-24 Related Antibodies

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Description

GPX4-IN-24 is an orally active glutathione peroxidase 4 (GPX4) inhibitor with a human IC50 of 10.90 μM, human Kd of 10.04 μM. GPX4-IN-24 suppresses GPX4 enzymatic activity, disrupts redox homeostasis, drives lipid peroxidation, promotes lipid peroxidation, and induces ferroptosis. GPX4-IN-24 can be used for the research of triple-negative breast cancer[1].

IC50 & Target[1]

GPX4

10.90 μM (IC50)

GPX4

10.04 μM (Kd)

In Vitro

GPX4-IN-24 (DA-5) binds directly to recombinant human GPX4 with a dissociation constant (Kd) of 10.04 μM[1].
GPX4-IN-24 (2.63-30 μM; 15 min) potently inhibits recombinant human GPX4 enzymatic activity with an IC50 of 10.90 μM[1].
GPX4-IN-24 (5 μM; 1 h) significantly inhibits GPX4 enzymatic activity in MDA-MB-231 triple-negative breast cancer cell lysates[1].
GPX4-IN-24 (1.25-20 μM; 72 h) selectively inhibits the proliferation of MDA-MB-231, MDA-MB-468, BT-549, and 4T1 TNBC cells while sparing SK-BR-3 non-TNBC cells and MCF10A normal mammary epithelial cells[1].
GPX4-IN-24 (2.5 μM; 7 days) suppresses colony formation in MDA-MB-231 and MDA-MB-468 TNBC cells but not in MCF10A normal mammary epithelial cells after 7-10 days of treatment[1].
GPX4-IN-24 (5 μM; 24 h) induces selective cell death in MDA-MB-231 TNBC cells while sparing MCF10A normal mammary epithelial cells[1].
GPX4-IN-24 (10 μM; 48 h) induces time-dependent lipid ROS accumulation in MDA-MB-231 TNBC cells, which is attenuated by ferroptosis inhibitors Ferrostatin-1 (HY-100579) and Liproxstatin-1 (HY-12726), while having no significant effect on lipid ROS levels in MCF10A normal mammary epithelial cells[1].
GPX4-IN-24 (5 μM; 24 h) alters the lipid profile of MDA-MB-231 TNBC cells, significantly upregulating ferroptosis-associated lipids including phosphatidic acid, phosphatidylethanolamine, phosphatidylinositol, and lysophospholipids[1].
GPX4-IN-24 (2.5-10 μM; 24 h) upregulates transferrin receptor 1 (TfR1) expression in MDA-MB-231 TNBC cells[1].

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

GPX4-IN-24 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231; MDA-MB-468; BT-549; 4T1; SK-BR-3; MCF10A
Concentration: 1.25 μM; 2.5 μM; 5 μM; 10 μM; 20 μM
Incubation Time: 72 h
Result: Exhibited strong antiproliferative effects against TNBC cell lines (MDA-MB-231, MDA-MB-468, BT-549, 4T1), with cell numbers reduced to 20% or less of control at 20 μM.
Had minimal effects on non-TNBC SK-BR-3 cells (cell numbers remaining ~80% of control at 20 μM) and normal MCF10A cells (cell numbers remaining ~100% of control across tested concentrations).

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231; MDA-MB-468; MCF10A
Concentration: 2.5 μM
Incubation Time: 7 days
Result: Drastically reduced colony formation in MDA-MB-231 and MDA-MB-468 TNBC cells, while having no significant effect on colony formation in MCF10A normal mammary epithelial cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231; MCF10A
Concentration: 5 μM
Incubation Time: 24 h
Result: Induced 50% cell death in MDA-MB-231 cells, compared to less than 9% cell death in MCF10A cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 2.5 μM; 5 μM; 10 μM
Incubation Time: 24 h
Result: Upregulated TfR1 protein expression in MDA-MB-231 cells in a concentration-dependent manner, with increased expression observed at 2.5, 5, and 10 μM compared to untreated control cells.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ T1/2 Tmax Vz/F CLz/F Cmax
Mice[1] 30 mg/kg p.o. 6937.5 μg/L·h 6938.81 μg/L·h 4.373 h 4.377 h 1.686 h 1 h 10.521 L/kg 4.324 L/h/kg 2030 μg/L
In Vivo

GPX4-IN-24 (DA-5) (30 mg/kg; p.o.; every 3 days for 24 days) significantly suppresses triple-negative breast cancer xenograft growth in female nude mice without systemic toxicity[1].

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

Animal Model: nude mice (6-8 weeks old, female; triple-negative breast cancer xenograft model via subcutaneous MDA-MB-231 cell injection)[1]
Dosage: 30 mg/kg
Administration: p.o.; every 3 days
Result: Significantly suppressed tumor growth, with mean tumor volume and tumor weight significantly lower than vehicle controls.
Did not affect mouse body weight.
Showed no hepatorenal toxicity via histopathological analysis.
Molecular Weight

569.65

Formula

C31H35N7O4
CAS No.
SMILES

O=C(C(NCCC1=NC=CC=C1)=O)C2=CNC(N=C3)=C2C=C3C4=CC=C(N5CCC(NC(OC(C)(C)C)=O)CC5)N=C4
Shipping

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-IN-24 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-IN-242834106-56-6Glutathione PeroxidaseFerroptosisReactive Oxygen Species (ROS)normal mammary epithelial cellsBT-549SK-BR-3glutathione peroxidase 4triple-negative breast cancer xenograftMCF10Atriple-negative breast cancer cells4T1MDA-MB-468MDA-MB-231Inhibitorinhibitorinhibit

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