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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3091513-13-9
- 分子式: C41H59N7O10
- 分子量:809.95
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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.
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Cell Line:MCF-7 cells
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Concentration:50 μM
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Incubation Time:24 h, 48 h
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Result:Had no significant antiproliferative activity when used alone, but combined with Artesunate or Palbociclib significantly enhanced the anti-cancer effects of both.
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Cell Line:MCF-7 cells, T47D cells
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Concentration:0.005 μM, 0.05 μM, 0.5 μM, 5 μM, 50 μM
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Incubation Time:12 h
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Result:Significantly degraded FTH1 protein.
Bearing L-tyrosine fragments, was more efficient than AY-7 bearing D-tyrosine fragments.
化学情報
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CAS 番号 3091513-13-9
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分子量 809.95
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分子式 C41H59N7O10
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)