Art. -Nr.: HY-141809

GPX4-IN-3

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM.

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Reinheit: 99.83%
CAS. Nr.: 2761004-85-5
Formel: C₂₉H₂₄ClN₃O₃S
Molecular Weight:530.04

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GPX4-IN-3 Chemical Structure

CAS. Nr.: 2761004-85-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM^[1].

IC₅₀ & Target

GPX4

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen :

GPX1
GPX4

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.78 μM Compound: 26a	Cytotoxicity against human 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34506134]
4T1	IC₅₀	0.78 μM Compound: 26a	Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34506134]
HT-1080	IC₅₀	0.15 μM Compound: 26a	Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34506134]
HT-1080	IC₅₀	4.73 μM Compound: 26a	Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs in presence of Fer-1 by MTT assay Cytotoxicity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs in presence of Fer-1 by MTT assay	[PMID: 34506134]
MCF7	IC₅₀	6.9 μM Compound: 26a	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34506134]

In Vitro

GPX4-IN-3 (26a) exhibits IC₅₀ values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively^[1].
GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3^[1].
GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity^[1].
GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity^[1].
GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1)^[1].

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

In Vivo

GPX4-IN-3 (26a) exertes antitumor activity and good biological safety in vivo^[1].

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

Animal Model:

Mouse 4T1 xenograft model^[1].
Dosage:

15 and 30 mg/kg.
Administration:

Intravenous injection, every two days for a total of five times.
Result:

Significantly suppress tumor growth with a tumor growth inhibition (TGI) value of 33.2 and 55.1% at 15 and 30 mg/kg, respectively.

Chemical Information

CAS. Nr. 2761004-85-5
Appearance Solid
Molecular Weight 530.04
Formel C₂₉H₂₄ClN₃O₃S
Color White to off-white
SMILES

O=C(C(C1=CSC2=CC=CC=C21)N(C3=CC=C(C=C3)C4=CN=CO4)C(CCl)=O)NCCC5=CC=CC=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Redox Biol

EGR1 regulates oxidative stress and aldosterone production in adrenal cells and aldosterone-producing adenomas. [Abstract]

2025 Mar:80:103498. PMID: 39826326
J Exp Clin Cancer Res

L-kynurenine induces NK cell loss in gastric cancer microenvironment via promoting ferroptosis. [Abstract]

2023 Mar 1;42(1):52. PMID: 36855135

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 67.5 mg/mL (127.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8867 mL

9.4333 mL

18.8665 mL

5 mM

0.3773 mL

1.8867 mL

3.7733 mL

10 mM

0.1887 mL

0.9433 mL

1.8867 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 6.75 mg/mL (12.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 6.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (67.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 6.75 mg/mL (12.73 mM); Clear solution

This protocol yields a clear solution of ≥ 6.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (67.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Congjun Xu, et al. Discovery of a Potent Glutathione Peroxidase 4 Inhibitor as a Selective Ferroptosis Inducer. J Med Chem. 2021 Sep 23;64(18):13312-13326. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.8867 mL	9.4333 mL	18.8665 mL	47.1663 mL
	5 mM	0.3773 mL	1.8867 mL	3.7733 mL	9.4333 mL
	10 mM	0.1887 mL	0.9433 mL	1.8867 mL	4.7166 mL
	15 mM	0.1258 mL	0.6289 mL	1.2578 mL	3.1444 mL
	20 mM	0.0943 mL	0.4717 mL	0.9433 mL	2.3583 mL
	25 mM	0.0755 mL	0.3773 mL	0.7547 mL	1.8867 mL
	30 mM	0.0629 mL	0.3144 mL	0.6289 mL	1.5722 mL
	40 mM	0.0472 mL	0.2358 mL	0.4717 mL	1.1792 mL
	50 mM	0.0377 mL	0.1887 mL	0.3773 mL	0.9433 mL
	60 mM	0.0314 mL	0.1572 mL	0.3144 mL	0.7861 mL
	80 mM	0.0236 mL	0.1179 mL	0.2358 mL	0.5896 mL
	100 mM	0.0189 mL	0.0943 mL	0.1887 mL	0.4717 mL

Keywords

GPX4-IN-3

2 Cited Publications

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GPX4-IN-3

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Anti-Cancer Metabolism Compound Library

Cuproptosis Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GPX4-IN-3

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GPX4-IN-3

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Anti-Cancer Metabolism Compound Library

Cuproptosis Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Radioprotector Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GPX4-IN-3

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GPX4-IN-3 Related Classifications

HY-141809 Related Classifications