Art. -Nr.: HY-175381

DeFer-2

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DeFer-2 is a ferritin PROTAC degrader (K_d = 17.1 μM). DeFer-2 induces ferritin degradation, triggering caspase 3-GSDME-mediated pyroptosis in cancer cells through free iron accumulation and elevated ROS. DeFer-2 significantly inhibits tumor growth and prolongs survival in mice bearing B16F10 subcutaneous tumors. DeFer-2 can be used to study melanoma.
(Pink: Ferritin ligand (HY-N1446); Blue: VHL ligand (HY-125845); Black: linker (HY-N0067)).

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Reinheit: 98.25%
CAS. Nr.: 3058911-16-0
Formel: C₄₄H₆₉N₅O₅S
Molecular Weight:780.11

Speicherung:

-20°C, stored under nitrogen

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

DeFer-2 Chemical Structure

CAS. Nr.: 3058911-16-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

DeFer-2 is a ferritin PROTAC degrader (K_d = 17.1 μM). DeFer-2 induces ferritin degradation, triggering caspase 3-GSDME-mediated pyroptosis in cancer cells through free iron accumulation and elevated ROS. DeFer-2 significantly inhibits tumor growth and prolongs survival in mice bearing B16F10 subcutaneous tumors. DeFer-2 can be used to study melanoma^[1]. (Pink: Ferritin ligand (HY-N1446); Blue: VHL ligand (HY-125845); Black: linker (HY-N0067)).

IC₅₀ & Target^[1]

VHL

Caspase 3

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

In Vitro

DeFer-2 (0-5 μM, 0-24 h) reduces the ferritin expression by forming a ternary complex with ferritin and VHL, induces disruption of redox and mitochondrial homeostasis in B16F10 cells^[1].
DeFer-2 (5 μM, 8-24 h) initiates caspase 3-GSDME-mediated pyroptosis through free iron accumulation and ROS elevation in B16F10 cells^[1].
DeFer-2 (24-48 h) causes severe cytotoxicity to B16F10 cells with IC₅₀s of 3.1 and 1.5 μM for 24 and 48 h, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

B16F10 cells
Concentration:

0, 0.008, 0.04, 0.2, 0.5, 1, 5 μM
Incubation Time:

0 h, 4 h , 8 h, 12 h, 16 h, 24 h
Result:

Reduced the ferritin expression.
Reduced the ferritin expression when as a nanoparticle albumin-DeFer-2.

Immunofluorescence^[1]

Cell Line:

B16F10 cells
Concentration:

5 μM
Incubation Time:

16 h
Result:

Increased ROS levels.

In Vivo

DeFer-2 (nanoparticle Albumin-DeFer-2, 10 mg/kg, i.v., every other day, 8 days) inhibits tumor growth and prolongs survival time in B16F10 tumor mice model^[1].

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

Animal Model:

B16F10 tumor (1 × 10⁶) mice (8-week-old, C57BL/6, male) model^[1]
Dosage:

10 mg/kg; in the form of nanoparticle albumin-DeFer-2
Administration:

i.v., every other day, 8 days
Result:

Inhibited tumor growth and prolonged survival time.
Did not cause systemic toxicity.

Chemical Information

CAS. Nr. 3058911-16-0
Appearance Solid
Molecular Weight 780.11
Formel C₄₄H₆₉N₅O₅S
Color Off-white to light yellow
SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(CCCNC(CCCCCCC/C=C\CCCCCCCC)=O)=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (128.19 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

1.2819 mL

6.4094 mL

12.8187 mL

5 mM

0.2564 mL

1.2819 mL

2.5637 mL

10 mM

0.1282 mL

0.6409 mL

1.2819 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 (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.

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 (3.20 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.20 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (3.20 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 (271 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]. Chen Y, et al. Small-Molecule Ferritin Degrader as a Pyroptosis Inducer. J Am Chem Soc. 2023 May 3;145(17):9815-9824. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2819 mL	6.4094 mL	12.8187 mL	32.0468 mL
	5 mM	0.2564 mL	1.2819 mL	2.5637 mL	6.4094 mL
	10 mM	0.1282 mL	0.6409 mL	1.2819 mL	3.2047 mL
	15 mM	0.0855 mL	0.4273 mL	0.8546 mL	2.1365 mL
	20 mM	0.0641 mL	0.3205 mL	0.6409 mL	1.6023 mL
	25 mM	0.0513 mL	0.2564 mL	0.5127 mL	1.2819 mL
	30 mM	0.0427 mL	0.2136 mL	0.4273 mL	1.0682 mL
	40 mM	0.0320 mL	0.1602 mL	0.3205 mL	0.8012 mL
	50 mM	0.0256 mL	0.1282 mL	0.2564 mL	0.6409 mL
	60 mM	0.0214 mL	0.1068 mL	0.2136 mL	0.5341 mL
	80 mM	0.0160 mL	0.0801 mL	0.1602 mL	0.4006 mL
	100 mM	0.0128 mL	0.0641 mL	0.1282 mL	0.3205 mL

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DeFer-2

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Pyroptosis Compound Library

PROTAC Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DeFer-2

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Pyroptosis Compound Library

PROTAC Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DeFer-2 Related Classifications

HY-175381 Related Classifications