ZD-1-186
ZD-1-186 is a non-degradative, covalent-dependent molecular glue that targets BCL6 and BRD9. ZD-1-186 inhibits the transcriptional output of MYC, relieves the repression of canonical BCL6 target loci (including CDKN1A (p21)), and mediates the selective recruitment of BRD9 to BCL6. ZD-1-186 can be used for research on diffuse large B-cell lymphoma.
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- 分子式: C35H37ClFN9O5S
- 分子量:750.24
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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 |
体外実験
ZD-1-186 (50 μM; 24 h) inhibits MYC protein levels and induces increased CDKN1A (p21) and BIM protein levels in SU-DHL-4 diffuse large B-cell lymphoma cells[1].
The MYC inhibition and CDKN1A (p21) induction mediated by ZD-1-186 (50 μM; 24 h) are attenuated in a dose-dependent manner by pharmacological inhibition of BRD9 with BI-9564 in HT diffuse large B-cell lymphoma cells[1].
The inhibitory effect of ZD-1-186 (50 μM; 24 h) on MYC in HT diffuse large B-cell lymphoma cells is attenuated by BRD9 knockout, whereas BRD9 knockout alone does not reduce MYC levels[1].
ZD-1-186 (50 μM; 24 h) simultaneously relieves the repression of the canonical BCL6 inhibitory site and suppresses MYC-driven transcriptional programs in HT diffuse large B-cell lymphoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 750.24
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分子式 C35H37ClFN9O5S
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SMILES
CNC(COC1=CC2=C(N(C)C1=O)C=CC(NC3=C(C=NC(N4CCN(C(/C=C/C(NC5=CC=C(C(F)=C5)N6CCSCC6)=O)=O)CC4)=N3)Cl)=C2)=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)
Keywords
- ZD-1-186
- Molecular Glues
- BCL6
- Epigenetic Reader Domain
- c-Myc
- B-cell lymphoma 6 protein
- B-cell lymphoma 5 protein (BCL-5)
- Zinc finger and BTB domain-containing protein 27
- Zinc finger protein 51
- Myc
- diffuse large B-cell lymphoma
- MYC
- CDKN1A (p21)
- BIM
- BRD9
- HT diffuse large B-cell lymphoma cells
- C288
- SU-DHL-4 diffuse large B-cell lymphoma cells
- HEK293T cells
- Inhibitor
- inhibitor
- inhibit