PROTAC FSP1 degrader 1
PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer.
(Pink: FSP1 ligand (HY-136057); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3096510-51-6
- Formula: C41H35N9O6
- Molecular Weight:749.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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ACSL4 |
Cereblon |
GPX4 |
PROTAC FSP1 degrader 1 (Compound 2307) (0-2 μM, 24 h) achieves an 83.2% degradation rate of FSP1 protein (DC50 = 263.7 nM) with no hook effect and demonstrates concentration-dependent degradation in MDA-MB-231 cells[1].
PROTAC FSP1 degrader 1 (1 μM, 24 h)-mediated degradation of FSP1 is significantly inhibited by pretreatment with MG132 (HY-13259), Pevonedistat (MLN4924) (HY-70062), and Pomalidomide (HY-10984) in MDA-MB-231 cells[1].
PROTAC FSP1 degrader 1 (0-100 μM, 24-48 h) does not show significant cytotoxicity against MDA-MB-231 cells when used alone (no significant decrease in cell viability), but it synergistically enhances cell death when used in combination with the GPX4 inhibitor RSL3[1].
PROTAC FSP1 degrader 1 (10 μM, 24 h) significantly reduces the proportion of EdU-positive cells and inhibits the proliferation of MDA-MB-231 cells[1].
PROTAC FSP1 degrader 1 (10 μM, 24 h) can induce the accumulation of ROS in MDA-MB-231 cells, initiating lipid peroxidation and ferroptosis[1].
PROTAC FSP1 degrader 1 (10 μM, 24 h) induces lipid peroxidation in MDA-MB-231 cells by degrading FSP1, a process that could be reversed by Fer-1, confirming the ferroptosis pathway[1].
PROTAC FSP1 degrader 1 (0.2-5 μM, 24 h) upregulates the mRNA expression of ferroptosis-related genes (GPX4, FTH1, ACSL4, TfR1, FSP1) in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:31.3 nM, 62.5 nM, 125 nM, 500 nM, 1000 nM, 2000 nM
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Incubation Time:24 h
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Result:Showed concentration-dependent degradation of FSP1 protein in MDA-MB-231 cells.
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Cell Line:MDA-MB-231 cells
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Concentration:0.2 μM, 1 μM, 5 μM
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Incubation Time:24 h
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Result:Upregulated the mRNA expression of ferroptosis-related genes (GPX4, FTH1, ACSL4, TfR1, FSP1) in MDA-MB-231 cells.
Chemical Information
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CAS No. 3096510-51-6
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Molecular Weight 749.77
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Formula C41H35N9O6
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SMILES
O=C(NC1=C(C#N)C(C2=CC=C(C)C=C2)=C(C#N)C3=NC4=CC=CC=C4N13)CC(NCCCCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O
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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)