SJH1-51B
SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research.
(Pink: BET ligand (HY-78695); Blue: SKP1 ligand (HY-175905); 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: C42H50ClN7O4S
- 分子量:784.41
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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 |
SKP1 |
体外実験
SJH1-51B (0.1-10 μM; 24 h) dose-dependently degrades the short isoform of BRD4 in HEK293T cells, with the most robust degradation at 10 μM, but does not affect the long BRD4 isoform[1].
SJH1-51B (0.1-10 μM; 24 h) dose-dependently degrades both the long and short isoforms of BRD4 in MDA-MB-231 cells, with the most robust degradation at 10 μM[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:HEK293T cells
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Concentration:0.1, 1, 5, 10 μM
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Incubation Time:24 h
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Result:Reduced short BRD4 levels to ~95% of vehicle control at 0.1 μM.
Reduced short BRD4 levels to ~50% of vehicle control at 1 μM.
Reduced short BRD4 levels to ~60% of vehicle control at 5 μM.
Reduced short BRD4 levels to ~20% of vehicle control at 10 μM.
Did not degrade the long BRD4 isoform.
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Cell Line:MDA-MB-231 breast cancer cells
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Concentration:0.1, 1, 5, 10 μM
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Incubation Time:24 h
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Result:Reduced long BRD4 levels to ~80% and short BRD4 levels to ~85% of vehicle control at 0.1 μM.
Reduced long BRD4 levels to ~80% and short BRD4 levels to ~70% of vehicle control at 1 μM.
Reduced long BRD4 levels to ~50% and short BRD4 levels to ~60% of vehicle control at 5 μM.
Reduced long BRD4 levels to ~30% and short BRD4 levels to ~10% of vehicle control at 10 μM.
化学情報
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分子量 784.41
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分子式 C42H50ClN7O4S
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SMILES
O=C(NCCCCNC(C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1)=O)CCCOC5=CC=CC(CC6CCN(C(C=C)=O)CC6)=C5
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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)
SJH1-51B 関連分類
HY-162240 関連分類
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