2. Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Cell Cycle/DNA Damage
  3. Glutathione Peroxidase Ferroptosis Lipoxygenase Reactive Oxygen Species (ROS) DNA/RNA Synthesis
  4. GPX4-IN-19

GPX4-IN-19 is an effective GPX4 inhibitor (IC50 = 0.311 μM), covalently binds to the Sec 46 site of GPX4. GPX4-IN-19 shows strong anti-proliferative activity with high ferroptosis selectivity. GPX4-IN-19 causes intracellular Fe2+ accumulation, leading to increased levels of lipid peroxides (LPOs) and reactive oxygen species (ROS), which induces ferroptosis and subsequently results in DNA damage. GPX4-IN-19 can be used for the study of Triple-Negative Breast Cancer (TNBC).

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

GPX4-IN-19

GPX4-IN-19 Chemical Structure

CAS No. : 3102894-57-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

GPX4-IN-19 Related Antibodies

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

GPX4-IN-19 is an effective GPX4 inhibitor (IC50 = 0.311 μM), covalently binds to the Sec 46 site of GPX4. GPX4-IN-19 shows strong anti-proliferative activity with high ferroptosis selectivity. GPX4-IN-19 causes intracellular Fe2+ accumulation, leading to increased levels of lipid peroxides (LPOs) and reactive oxygen species (ROS), which induces ferroptosis and subsequently results in DNA damage. GPX4-IN-19 can be used for the study of Triple-Negative Breast Cancer (TNBC)[1].

In Vitro

GPX4-IN-19 (Compound Y19) (72 h) exhibits effective anti-proliferative activity to six cancer cell lines (MCF-7, MDA-MB-231, PC-3, MDA-MB-468, PANC-1, and ASPC-1) (IC50: 0.021-0.094 μM)[1].
GPX4-IN-19 (12.5-50 nM, 2 weeks) can effectively inhibit cell proliferation, and the addition of the inhibitor Ferrostatin-1 (HY-100579) (Fer-1) reversed the inhibition of cell proliferation in MDA-MB-231 cells[1].
GPX4-IN-19 (50 nM, 8 h) can cause mitochondria in the cells to show typical morphological changes, such as rupture of the outer mitochondrial membrane, smaller mitochondrial volume, and reduction or absence of inner mitochondrial crista in MDA-MB-231 cells[1].
GPX4-IN-19 (12.5-50 nM, 8 h) induces dose-dependent increases in intracellular Fe2+ concentration, LPOs accumulation, MDA content, and ROS level in MDA-MB-231 cells[1].
GPX4-IN-19 (12.5-50 nM, 8 h) causes DNA damage in MDA-MB-231 cells by increasing the expression of γH2AX, and this DNA damage is significantly attenuated by the addition of inhibitors such as Fer-1[1].
GPX4-IN-19 (1 μM, 2 h) reduces the degradation temperature of GPX4 protein at the same temperature in MDA-MB-231 cells, indicating that GPX4-IN-19 reduced the thermal stability of GPX4 protein[1].
GPX4-IN-19 (12.5 nM, 25 nM, 50 nM, 8 h) exhibits significant resistance in the MDA-MB-231 cell lines that are resistant to GPX4 inhibitors RSL3 or ML162 (MDA-MB-231-RSL3 and MDA-MB-231-ML162)[1].
GPX4-IN-19 (12.5-50 nM, 4-12 h) reduces GPX4 levels in a concentration-dependent manner in MDA-MB-231 cells. However, time-course analysis reveals that GPX4 expression initially increases at 4 hours, with minimal change in xCT levels at this early time point, but subsequently decreases at 8 hours accompanied by a significant increase in xCT expression[1].

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

GPX4-IN-19 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 2 weeks
Result: Effectively inhibited cell proliferation, and the addition of the inhibitor Fer-1 reversed the inhibition of cell proliferation in MDA-MB-231 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 8 h
Result: Increased expression of DNA damage marker γH2AX.
Decreased the level of GPX4 in a concentration-dependent manner.
Didn't inhibit other proteins contained selenium, including Glutathione peroxidase 1 (GPX1) and Thioredoxin reductase 1 (TXNRD1).
FTH1 was significantly decreased with the concentration change.
Increased ACSL4 expression levels.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 8 h
Result: Reduced GPX4 level in a concentration-dependent manner in MDA-MB-231 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 4 h, 8 h, 12 h
Result: The expression of GPX4 increased at 4 h, and the xCT level of the upstream signaling pathway hardly changed at this time, but the expression level of GPX4 decreased and the expression level of xCT increased at 8h.
In Vivo

GPX4-IN-19 (5 mg/kg, 10 mg/kg, i.p., every two days for 24 days) demonstrates a dose-dependent antitumor effect in the MDA-MB-231 tumor-bearing mouse model without causing significant weight loss, abnormal blood biochemical indicators, or organ pathological damage, showing good safety characteristics[1].

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

Animal Model: MDA-MB-231 cells (1 × 107 cells in 200 μL suspension, mixed 1:1 with Matrigel and PBS) are subcutaneously injected into the left flank of female BALB/c nude mice (4 to 5weeks old)[1].
Dosage: 5 mg/kg, 10 mg/kg
Administration: I.p., every two days for 24 days
Result: Tumor growth was inhibited in a dose-dependent manner, tumor growth inhibition (TGI) of 72.53 % at 10 mg/kg.
Ki67-positive tumor cells were decreased.
GPX4 was significantly decreased compared with the control group.
Revealed no apparent morphological abnormalities in major organs, including the heart, liver, spleen, lungs, and kidneys.
Could not destroy the function of the liver, the kidneys, and the heart.
Molecular Weight

395.81

Formula

C19H19ClFNO5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=CC(N(C(CCl)=O)CC2=CC3=C(OCCO3)C=C2)=CC(OC)=C1F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (126.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5265 mL 12.6323 mL 25.2646 mL
5 mM 0.5053 mL 2.5265 mL 5.0529 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5265 mL 12.6323 mL 25.2646 mL 63.1616 mL
5 mM 0.5053 mL 2.5265 mL 5.0529 mL 12.6323 mL
10 mM 0.2526 mL 1.2632 mL 2.5265 mL 6.3162 mL
15 mM 0.1684 mL 0.8422 mL 1.6843 mL 4.2108 mL
20 mM 0.1263 mL 0.6316 mL 1.2632 mL 3.1581 mL
25 mM 0.1011 mL 0.5053 mL 1.0106 mL 2.5265 mL
30 mM 0.0842 mL 0.4211 mL 0.8422 mL 2.1054 mL
40 mM 0.0632 mL 0.3158 mL 0.6316 mL 1.5790 mL
50 mM 0.0505 mL 0.2526 mL 0.5053 mL 1.2632 mL
60 mM 0.0421 mL 0.2105 mL 0.4211 mL 1.0527 mL
80 mM 0.0316 mL 0.1579 mL 0.3158 mL 0.7895 mL
100 mM 0.0253 mL 0.1263 mL 0.2526 mL 0.6316 mL
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GPX4-IN-19 Related Classifications

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-193102894-57-2Glutathione PeroxidaseFerroptosisLipoxygenaseReactive Oxygen Species (ROS)DNA/RNA SynthesisLOXCovalent inhibitorsGlutathione peroxidase 4Lipid peroxidationInhibitorinhibitorinhibit

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