BiBET
BiBET is a selective BRD4 inhibitor with a pKd of 11 for BRD4 (1,2). BiBET downregulates c-Myc. BiBET can be used in cancer research.
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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: 2059110-46-0
- 分子式: C26H30N10O3
- 分子量:530.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
BRD4(BD1BD2) 11 (pKd) |
BRD4(1) 8.1 (pKd) |
BRD4(2) 7.3 (pKd) |
体外実験
BiBET (1 mM) induces conformational compaction of BRD4(1,2), producing a faster-sedimenting species with s20,w = 2.8 S at 1:1 and dimeric species at 2:1[1].
BiBET (1 μM) is selective for BET BRDs and shows no detectable kinase activity at 1 μM, with the most potent off-target 5HT1B EC50 = 0.93 μM[1].
BiBET (50 nM) downregulates c-Myc in MM.1S cells with pEC50 = 9.2 and maintains knockdown for 16 h after washout[1].
BiBET (0.05 μM; 24 h) induces transcriptional changes in K-562, MM.1S, and MV-4-11 cells that are highly correlated with BET inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S
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Concentration:50 nM
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Incubation Time:2, 4, 16 h after compound washout
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Result:Downregulated c-Myc.
化学情報
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CAS 番号 2059110-46-0
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分子量 530.58
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分子式 C26H30N10O3
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SMILES
CN(CCOC1=CC=C(C2CCN(C3=NN4C(C=C3)=NN=C4OC)CC2)C=C1)C5=NN6C(C=C5)=NN=C6OC
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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)