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^[1]. (Pink: FSP1 ligand (HY-136057); Blue: Cereblon ligand (HY-10984); Black: linker).

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.

749.77

C₄₁H₃₅N₉O₆

3096510-51-6

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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• [1]. Huang Y, et al. Design, synthesis, and induction of tumor ferroptosis activity of a novel FSP1 protein degrading agent. Eur J Med Chem. 2026 Jan 15;302(Pt 1):118270.  [Content Brief]