PROTAC GPX4 degrader-1

Name: PROTAC GPX4 degrader-1
Brand: MedChemExpress
SKU: HY-149236
Rating: 4.5 (0 reviews)

製品番号: HY-149236 純度: 99.35%: Data Sheet SDS COA 取扱説明書
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Technical Support

PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC₅₀ of 0.03 μM in HT1080 cells.

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PROTAC GPX4 degrader-1 構造式

CAS 番号 : 2916433-81-1

容量	価格（税別）	在庫状況	数量
1 mg	$850	在庫あり	Estimated Time of Arrival: December 31
5 mg	$2133	在庫あり	Estimated Time of Arrival: December 31
10 mg	$3200	在庫あり	Estimated Time of Arrival: December 31
50 mg		お問い合わせ
100 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Glutathione Peroxidase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

GPX1 GPX4

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC₅₀ of 0.03 μM in HT1080 cells^[1].

IC₅₀ & Target

GPX4

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.2 μM Compound: DC-2	Antiproliferative activity against human A-375 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human A-375 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 37087895]
Calu-1	IC₅₀	0.3 μM Compound: DC-2	Antiproliferative activity against human Calu-1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human Calu-1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 37087895]
HEK-293T	IC₅₀	1.1 μM Compound: DC-2	Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 37087895]
HT-1080	IC₅₀	0.1 μM Compound: DC-2	Antiproliferative activity against human HT-1080 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HT-1080 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 37087895]

体外実験

PROTAC GPX4 degrader-1 (DC-2) has been found to induce GPX4 degradation and subsequent ferroptosis^[1].

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

Western Blot Analysis^[1].

Cell Line:	HT1080 cells.
Concentration:	0.003-1 μM.
Incubation Time:	24 h.
Result:	Dose-dependently degraded GPX4 protein levels.

分子量

993.50

分子式

C₅₀H₅₇ClN₁₀O₁₀

CAS 番号

2916433-81-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1CCN(C(C2=CC=C(C=C2)OCC(N3CCC(CC3)CN4CCN(CCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)CC4)=O)C8=CC=C(C=C8)Cl)CC1)C9=NOC(C)=C9[N+]([O-])=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (100.65 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	1.0065 mL	5.0327 mL	10.0654 mL
5 mM	0.2013 mL	1.0065 mL	2.0131 mL
10 mM	0.1007 mL	0.5033 mL	1.0065 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 (stored under nitrogen). 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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.52 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.52 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 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.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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.

純度とドキュメンテーション

純度: 99.35%

Select Batch:

データシート (271 KB) SDS (252 KB)

COA (246 KB) HNMR (375 KB) RP-HPLC (206 KB) LCMS (96 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Han Wang, et al. Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells. Eur J Med Chem. 2023 Jun 5;254:115343. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0065 mL	5.0327 mL	10.0654 mL	25.1636 mL
	5 mM	0.2013 mL	1.0065 mL	2.0131 mL	5.0327 mL
	10 mM	0.1007 mL	0.5033 mL	1.0065 mL	2.5164 mL
	15 mM	0.0671 mL	0.3355 mL	0.6710 mL	1.6776 mL
	20 mM	0.0503 mL	0.2516 mL	0.5033 mL	1.2582 mL
	25 mM	0.0403 mL	0.2013 mL	0.4026 mL	1.0065 mL
	30 mM	0.0336 mL	0.1678 mL	0.3355 mL	0.8388 mL
	40 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6291 mL
	50 mM	0.0201 mL	0.1007 mL	0.2013 mL	0.5033 mL
	60 mM	0.0168 mL	0.0839 mL	0.1678 mL	0.4194 mL
	80 mM	0.0126 mL	0.0629 mL	0.1258 mL	0.3145 mL
	100 mM	0.0101 mL	0.0503 mL	0.1007 mL	0.2516 mL