FD1-C10-CB
FD1-C10-CB is a PROTAC degrader targeting the BRD4 protein. FD1-C10-CB binds to FEM1B to form a ternary complex with BRD4, achieving FEM1B-dependent degradation of BRD4 via the ubiquitin-proteasome system. FD1-C10-CB binds to CD36 to mediate endocytic cellular delivery, thereby enhancing its degrading activity. FD1-C10-CB mediates protein degradation through the Cullin-dependent ubiquitin-proteasome pathway, rather than the lysosomal autophagy pathway. FD1-C10-CB induces a decrease in BRD4 protein levels, and its degrading activity is competitively inhibited by FL47 or JQ1. FD1-C10-CB can be used in the research of breast cancer and osteosarcoma.
(Pink: BRD4 ligand (HY-78695); Blue: FEM1B E3 ligase ligand; Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C64H85Cl2N9O9S
- 分子量:1227.39
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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
製品説明
IC50 & Target
[1]|
BRD4 |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells, FEM1B-knockout HEK293T cells
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Concentration:10 μM (inhibitor/competitor experiments); multiple concentrations (dose-dependent analysis)
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Incubation Time:1-24 h
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Result:Induced concentration- and time-dependent degradation of BRD4, with significantly improved DC50 and Dₘₐₓ values compared to the parent compound FD1.
Abrogated BRD4 degradation in FEM1B-knockout cells.
Inhibited BRD4 degradation when co-administered with proteasome inhibitor MG132, neddylation inhibitor MLN4924, CD36 inhibitor SMS121, and excess FL47 or JQ1.
Left BRD4 degradation unaffected by lysosomal inhibitors bafilomycin A1 or chloroquine.
化学情報
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分子量 1227.39
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分子式 C64H85Cl2N9O9S
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SMILES
ClCC(N1CCN(CCCNC([C@]23C[C@@H]4C[C@@H](C[C@@](C(NC5=CC(OCCNC(C[C@H]6C7=NN=C(C)N7C(SC(C)=C8C)=C8C(C9=CC=C(Cl)C=C9)=N6)=O)=CC(OC(CCCCCCCCCCC(OC(C)(C)C)=O)=O)=C5)=O)(C4)C3)C2)=O)CC1)=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)