DA-PROTAC
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research.
(Pink: ATOX1 and CCS ligand (HY-184970); Blue: VHL ligand (HY-184971); Black: linker (HY-48450)).
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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: 2488660-12-2
- 分子式: C46H50BrF2N7O8S2
- 分子量:1010.96
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
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VHL |
体外実験
DA-PROTAC (0-1 μM, 24 h) can degrade Atox1 and CCS proteins rather than inhibit Atox1 and CCS activity[1].
DA-PROTAC (5 μM, 24 h) inhibits the proliferation, migration and invasion of triple negative breast cancer cells (MDA-MB-231)[1].
DA-PROTAC (10 μM, 48 h) inhibits the tumorigenic capacity of triple negative breast cancer cells (MDA-MB-231)[1].
The targeting module of DA-PROTAC is a small molecule VHL ligand1 combined with E3 ligase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231 cells
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Concentration:100 nM ,200 nM ,500 nM , and 1000 nM
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Incubation Time:24 h
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Result:Significantly reduced ATOX1 and CCS protein levels under 200nM, indicating that DA-PROTAC can degrade ATOX1 and CCS proteins.
化学情報
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CAS 番号 2488660-12-2
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分子量 1010.96
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分子式 C46H50BrF2N7O8S2
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SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)C(C(C)(C)C)NC(COCCCOCC(NC4=C(C(NC5=C(C=C(C=C5F)F)Br)=O)SC6=C4C=C(CCC7)C7=N6)=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.
プロトコル
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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)