2. PROTAC Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease NF-κB
  3. PROTACs Pyroptosis Reactive Oxygen Species (ROS) Caspase
  4. DeFer-2

DeFer-2 is a ferritin PROTAC degrader (Kd = 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: Oleic acid: HY-N1446, Blue: (S,R,S)-AHPC: HY-125845, Black: γ-Aminobutyric acid: HY-N0067, Blue + Black: (S,R,S)-AHPC-C3-NH2: HY-130711).

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DeFer-2

DeFer-2 Chemical Structure

CAS No. : 3058911-16-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

DeFer-2 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Caspase Isoform Specific Products:

View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DeFer-2 is a ferritin PROTAC degrader (Kd = 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: Oleic acid: HY-N1446, Blue: (S,R,S)-AHPC: HY-125845, Black: γ-Aminobutyric acid: HY-N0067, Blue + Black: (S,R,S)-AHPC-C3-NH2: HY-130711)[1].

IC50 & Target[1]

VHL

 

Caspase 3

 

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.

DeFer-2 Related Antibodies

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.
Molecular Weight

780.11

Formula

C44H69N5O5S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2819 mL 6.4094 mL 12.8187 mL
5 mM 0.2564 mL 1.2819 mL 2.5637 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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    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.

    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 (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.

    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)

g

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.
Purity & Documentation
References

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.

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 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:

DeFer-23058911-16-0DeFer2DeFer 2PROTACsPyroptosisReactive Oxygen Species (ROS)CaspaseDegradermelanomaB16F10 cellspyroptosisB16F10 tumor miceInhibitorinhibitorinhibit

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