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

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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.

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.
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

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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DeFer-2
Cat. No.:
HY-175381
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