GPX4-IN-3

Name: GPX4-IN-3
Brand: MedChemExpress
SKU: HY-141809
Rating: 4.5 (1 reviews)

Cat. No.: HY-141809 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

GPX4-IN-3 Chemical Structure

CAS No. : 2761004-85-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 257	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 257	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 840	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1340	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2140	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE GPX4-IN-3

•J Exp Clin Cancer Res. 2023 Mar 1;42(1):52. [Abstract]

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Biological Activity
Purity & Documentation
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Description

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].

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]
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.

Molecular Weight

530.04

Formula

C₂₉H₂₄ClN₃O₃S

CAS No.

2761004-85-5

Appearance

Solid

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

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 : 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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (256 KB) HNMR (382 KB) RP-HPLC (243 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

GPX4-IN-3 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-32761004-85-5Glutathione PeroxidaseFerroptosisGlutathionePeroxidasegpx4ferroptosisLPOROSInhibitorinhibitorinhibit

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GPX4-IN-3

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GPX4-IN-3 Related Antibodies

1 Publications Citing Use of MCE GPX4-IN-3

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GPX4-IN-3 Related Antibodies

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Complete Stock Solution Preparation Table

GPX4-IN-3 Related Classifications

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