Art. -Nr.: HY-155663

GPX4-IN-5

Name: GPX4-IN-5
Brand: MedChemExpress
SKU: HY-155663
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GPX4-IN-5 is a covalent inhibitor of GPX4 (IC₅₀: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC).

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Reinheit : 99.73%
CAS. Nr.: 2922824-09-5
Formel: C₁₈H₁₇ClFNO₅
Molecular Weight:381.78

Speicherung:

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

GPX4-IN-5 Chemical Structure

CAS. Nr.: 2922824-09-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

GPX4

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen :

GPX1
GPX4

Cellular Effect

Cell Line	Type	Value	Description	References
BT-549	IC₅₀	0.075 μM Compound: C18	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	>20 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of glutathione by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of glutathione by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	>20 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of N-acetyl-L-cysteine by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of N-acetyl-L-cysteine by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	0.012 μM Compound: C18	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	0.018 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of autophagy inhibitor, 3-MA by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of autophagy inhibitor, 3-MA by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	0.022 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of necrosis inhibitor, necrostatin-1 by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of necrosis inhibitor, necrostatin-1 by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	0.031 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of apoptosis inhibitor, Z-VAD-FMK by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of apoptosis inhibitor, Z-VAD-FMK by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	2.57 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of deferoxamine by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of deferoxamine by MTT assay	[PMID: 37452764]
MDA-MB-231	IC₅₀	2.57 μM Compound: C18	Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of ferroptosis inhibitor, ferrostatin-1 by MTT assay Induction of ferroptosis in human MDA-MB-231 cells assessed as cell viability incubated for 72 hrs in presence of ferroptosis inhibitor, ferrostatin-1 by MTT assay	[PMID: 37452764]
MDA-MB-468	IC₅₀	0.01 μM Compound: C18	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 37452764]

In Vitro

GPX4-IN-5 (Compound 18) (72 hours) has antitumor activity against TNBC cells (MDA-MB-468, BT-549, MDA-MB-468) with IC₅₀s of 0.01, 0.075, and 0.012 μM, respectively.
GPX4-IN-5 (1 μM, 72 hours) is unable to effectively kill MDA-MB-231 cells induced by ferroptosis inhibitors (Ferrostatin-1 (HY-100579), Acetylcysteine (HY-B0215), L-Glutathione reduced (HY-D0187)), indicating that it relies on ferroptosis to exert its potent cell-killing effect^[1].
GPX4-IN-5 (5-20 nM, 8 hours) increases Fe²⁺ and ROS levels in MDA-MB-231 cells, leading to LPOs accumulation and inducing ferroptosis^[1].
GPX4-IN-5 (20 nM, 6 hours) causes mitochondrial volume reduction, cristae disappearance, and outer membrane rupture in MDA-MB-231 cells, which are consistent with the characteristics of ferroptosis^[1].
GPX4-IN-5 (1 hour) has significant inhibitory activity against GPX4 (IC₅₀: 0.12 μM)^[1].
GPX4-IN-5 (1 μM, 2 hours) decreases the degradation temperature of GPX4 in MDA-MB-231 cells as determined by Celular Thermal shift Assay, indicating that it can directly bind to GPX4^[1].
GPX4-IN-5 (50-800 nM, 90 minutes) has a strong covalent bond formation ability with GPX4 (K_inact/K_I: 93.54 min/M)^[1].
GPX4-IN-5 (20 nM) slightly increases LPO in MDA-MB-231 cells transfected with siGPX4#1, and the levels of GPX4-related proteins does not change significantly, indicating that it induces cell ferroptosis by specifically targeting GPX4 protein^[1].
GPX4-IN-5 (5-20 nM, 10 hours) inhibits GPX4 activity rather than downregulating GPX4 levels to induce ferroptosis in MDA-MB-231 cells^[1].

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

Western Blot Analysis

Cell Line:

MDA-MB-231 cells
Concentration:

5, 10, 20 nM
Incubation Time:

4, 6 8, 10 h
Result:

Showed a decrease in the expression levels of negative regulatory proteins of ferroptosis (GPX4 and FTH1), and the decrease in FTH1 was associated with abnormal iron metabolism.
Showed that the expression level of the xCT system was not downregulated, indicating that it was not inhibited.
Caused a compensatory upregulation of GPX4 expression within 6 hours, and then decreased after 8 hours.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	Plasma Concentration	AUC	MRT	Clearance (CL)
Rat^[1]	10 mg/kg	i.p.	1.90 h	0.85 h	5205 ng/mL	12.099 ng·h/mL	1.71 h	0.83 L/h/kg

In Vivo

GPX4-IN-5 (Compound 18) (5-20 mg/kg, i.p., once a day for 21 consecutive days) has significant anti-tumor activity in the MDA-MB-231 xenograft tumor BALB/C nude mouse model, and has no obvious damage to kidney, liver and heart function^[1].
GPX4-IN-5 (20 mg/kg, i.p., once a day for 14 consecutive days) has no obvious blood toxicity, does not cause bone marrow suppression, and has no obvious damage to kidney, liver and heart function in the BALB/C nude mouse model^[1].

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

Animal Model:

BALB/c nude mice (female, aged 4 weeks) injected with MDA-MB-231 (8 million cells)^[1]
Dosage:

5, 10, 20 mg/kg
Administration:

i.p. once a day, 21 consecutive days
Result:

Showed excellent tumor growth inhibition (TGI) ranging from 50.4% to 81.0%.
Showed no obvious drug-related damage in organs such as heart, liver, spleen, lung and kidney.
Can significantly reduce the level of GPX4 protein in tumor tissues, indicating that it can effectively induce ferroptosis in vivo.
Reduced the number of Ki67-positive tumor cells and inhibited the proliferation of tumor cells.

Animal Model:

BALB/c nude mice (female, aged 4 weeks)^[1]
Dosage:

20 mg/kg
Administration:

i.p. once a day, 14 consecutive days
Result:

Showed no significant differences in ALT, AST, BUN, CREA, LDH, and CK, indicated that the kidney, liver, and heart functions of the mice were not significantly damaged.
Has no obvious blood toxicity and did not cause bone marrow suppression, which is manifested by no significant changes in white blood cells (WBC), red blood cells (RBC) and hemoglobin (HGB).

Chemical Information

CAS. Nr. 2922824-09-5
Appearance Solid
Molecular Weight 381.78
Formel C₁₈H₁₇ClFNO₅
Color White to light brown
SMILES

COC1=CC(N(C2=CC3=C(OCCO3)C=C2)C(CCl)=O)=CC(OC)=C1F
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 (1)

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Journal Impact Factor

bioRxiv

2025 Jun 27.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (261.93 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

2.6193 mL

13.0965 mL

26.1931 mL

5 mM

0.5239 mL

2.6193 mL

5.2386 mL

10 mM

0.2619 mL

1.3097 mL

2.6193 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (284 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Chen T, et al. Discovery of Novel Potent Covalent Glutathione Peroxidase 4 Inhibitors as Highly Selective Ferroptosis Inducers for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2023 Jul 27;66(14):10036-10059. [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	2.6193 mL	13.0965 mL	26.1931 mL	65.4827 mL
	5 mM	0.5239 mL	2.6193 mL	5.2386 mL	13.0965 mL
	10 mM	0.2619 mL	1.3097 mL	2.6193 mL	6.5483 mL
	15 mM	0.1746 mL	0.8731 mL	1.7462 mL	4.3655 mL
	20 mM	0.1310 mL	0.6548 mL	1.3097 mL	3.2741 mL
	25 mM	0.1048 mL	0.5239 mL	1.0477 mL	2.6193 mL
	30 mM	0.0873 mL	0.4366 mL	0.8731 mL	2.1828 mL
	40 mM	0.0655 mL	0.3274 mL	0.6548 mL	1.6371 mL
	50 mM	0.0524 mL	0.2619 mL	0.5239 mL	1.3097 mL
	60 mM	0.0437 mL	0.2183 mL	0.4366 mL	1.0914 mL
	80 mM	0.0327 mL	0.1637 mL	0.3274 mL	0.8185 mL
	100 mM	0.0262 mL	0.1310 mL	0.2619 mL	0.6548 mL

Bioz

Keywords

GPX4-IN-5

1 Cited Publications

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GPX4-IN-5

Publications Citing Use of MedChemExpress (MCE) GPX4-IN-5

Alle Glutathione Peroxidase Isoform-spezifische Produkte anzeigen