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  3. AY-4

AY-4 (Compound AY-4) is an efficient PROTAC degrader targeting FTH1 (Kd = 3.17 nM). AY-4 effectively upregulates the levels of ferrous (Fe2+) and ferric (Fe3+) ions in cells. AY-4 is a potential anticancer candidate compound that regulates iron homeostasis through ferritin degradation and enhances the efficacy of existing drugs. AY-4 can effectively reduce the level of FTH1 in breast cancer cells (Pink: FTH1 ligand AY-2 (HY-174871); Blue: E3 ligand Pomalidomide (HY-10984); Black: Linker, Pomalidomide-PEG3-acid (HY-174872)).

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AY-4 Chemical Structure

AY-4 Chemical Structure

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Description

AY-4 (Compound AY-4) is an efficient PROTAC degrader targeting FTH1 (Kd = 3.17 nM). AY-4 effectively upregulates the levels of ferrous (Fe2+) and ferric (Fe3+) ions in cells. AY-4 is a potential anticancer candidate compound that regulates iron homeostasis through ferritin degradation and enhances the efficacy of existing drugs. AY-4 can effectively reduce the level of FTH1 in breast cancer cells (Pink: FTH1 ligand AY-2 (HY-174871); Blue: E3 ligand Pomalidomide (HY-10984); Black: Linker, Pomalidomide-PEG3-acid (HY-174872))[1].

In Vitro

AY-4 (Compound AY-4) (50 μM, 24-48 h) enhances the efficacy of Artesunate (HY-N0193) and Palbociclib (HY-50767) by releasing iron ions in MCF-7 cells[1].

AY-4 (50 μM, 12 h) is a highly effective FTH1 degrader in MCF-7 and T47D cells[1].

AY-4 (0.005-50 μM, 12 h) requires the L-configuration of its ligand to degrade FTH1[1].

AY-4 (50 μM) can increase intracellular ferrous ion (Fe2+) levels without inducing significant oxidative stress[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MCF-7 cells
Concentration: 50 μM
Incubation Time: 24 h, 48 h
Result: Had no significant antiproliferative activity when used alone, but combined with Artesunate or Palbociclib significantly enhanced the anti-cancer effects of both.

Western Blot Analysis[1]

Cell Line: MCF-7 cells, T47D cells
Concentration: 0.005 μM, 0.05 μM, 0.5 μM, 5 μM, 50 μM
Incubation Time: 12 h
Result: Significantly degraded FTH1 protein.
Bearing L-tyrosine fragments, was more efficient than AY-7 bearing D-tyrosine fragments.
Molecular Weight

809.95

Formula

C41H59N7O10

SMILES

NCCCNCCCCCCCCNC([C@@H](NC(COCCOCCOCCNC1=CC=CC2=C1C(N(C2=O)C3CCC(NC3=O)=O)=O)=O)CC4=CC=C(C=C4)O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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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Product Name:
AY-4
Cat. No.:
HY-174867
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