PROTAC GPX4 degrader-2
PROTAC GPX4 degrader-2 is a cIAP-recruiting GPX4 PROTAC degrader with a DC50 of 1.68 μM. PROTAC GPX4 degrader-2 forms a ternary complex with GPX4 and cIAP, and induces GPX4 degradation via the ubiquitin-proteasome system pathway. PROTAC GPX4 degrader-2 induces Mitochondrial depolarization and Ferroptosis. PROTAC GPX4 degrader-2 exhibits antiproliferative effects in cancer cells. PROTAC GPX4 degrader-2 can be used for the research of fibrosarcoma.
(Pink: GPX4 ligand (HY-175903); Blue: IAP ligand (HY-137159); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3035509-76-0
- Formula: C50H61ClN8O9
- Molecular Weight:953.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GPX4 1.68 μM (DC50) |
cIAP |
PROTAC GPX4 degrader-2 (Compound 18a) (0.1-10 μM; 12-72 h) potently degrades GPX4 in HT1080 cells, with a DC50 of 1.68 μM (48 h); this process relies on a mechanism of ternary complex formation with GPX4 and cIAP, and involves the ubiquitin-proteasome system[1].
PROTAC GPX4 degrader-2 (48 h) inhibits the proliferation of HT1080 cells with an IC50 of 2.37 μM, and this effect is mediated by inducing ferroptosis rather than apoptosis[1].
PROTAC GPX4 degrader-2 (0.6-10 μM) induces concentration-dependent accumulation of lipid peroxides in HT1080 cells, which is a hallmark feature of ferroptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT1080 human fibrosarcoma cells
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Concentration:0.1-10 μM (48 h incubation); 5 μM (12-72 h incubation; 48 h incubation with pre-treatment; 24 h incubation with washout)
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Incubation Time:12-72 h (5 μM concentration); 48 h (0.1-10 μM concentration; 5 μM with pre-treatment); 24 h (5 μM with washout) plus 6-24 h recovery
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Result:Induced concentration-dependent degradation of GPX4 with a DC50 (48 h) of 1.68 μM and a maximum degradation (Dₘₐₓ, 48 h) of 85%.
Caused time-dependent degradation, with significant reduction in GPX4 protein observed within 12 h of treatment with 5 μM, and maximum depletion achieved by 48 h.
Showed degradation effect that persisted for up to 12 h after compound washout.
Had GPX4 degradation blocked by pre-treatment with proteasome inhibitor MG132, neddylation inhibitor MLN4924, GPX4 inhibitor RSL3, or cIAP ligand B4.
Chemical Information
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CAS No. 3035509-76-0
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Molecular Weight 953.52
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Formula C50H61ClN8O9
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SMILES
O=C(NCC1=CN(CCCCCCCC(N[C@@H]([C@H](O)C(N[C@@H](CC(C)C)C(OC)=O)=O)CC2=CC=CC=C2)=O)N=N1)C(C=C3)=CC=C3[C@H](N(C(CCl)=O)[C@@H](C(OC)=O)C4)C5=C4C6=CC=CC=C6N5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC GPX4 degrader-2 Related Classifications
HY-162106 Related Classifications
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