EBET-1055
EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures.
(Pink: BET ligand (HY-161387); Blue: Cereblon ligand (HY-14658); 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: C51H54N8O9
- 分子量:923.02
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
EBET-1055 (1 nM, 10 nM; 2 d) inhibits CAF-induced IL-6 and LIF secretion when co-cultured with mouse CAF and PC-3 or PC-42 cancer cells[1].br /EBET-1055 has potential anti-inflammatory or anti-fibrotic activity. STAT3 signaling mediates the inflammatory CAF (iCAF) phenotype, and SMAD signaling mediates the myofibroblast CAF (myCAF) phenotype; and EBET-1055 (1-100 nM; 24 h) may inhibit the interaction of BRD proteins with STAT3 and SMAD3 It inhibits myofibroblast differentiation and reduces the phosphorylation levels of SMAD3 and STAT3 in mouse fibrotic kidneys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3 cells or mouse CAFs
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Concentration:0.1, 1, 10, 100 nM
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Incubation Time:24 h
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Result:Decreased the phosphorylation levels of STAT3Y705, SMAD2S465/467, and SMAD3S423/425 24 h after addition.
化学情報
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分子量 923.02
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分子式 C51H54N8O9
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SMILES
OC[C@](OC1CC1)(C2=CC=CC=C2)C3=NC(N4CCC(CN5CCN(C(COC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O)=O)CC5)CC4)=NC9=CC=C(C(C=C%10C)=CN(C)C%10=O)C=C93
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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
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データシート (268 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
EBET-1055 関連分類
HY-161346 関連分類
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