dBET1
产品编号: DC12023
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应用领域
dBET1 是基于 PROTAC 技术的有效的 BRD4 蛋白质降解物，其 EC50 值为 430 nM。dBET1 是一种由 BRD4 抑制剂 JQ1 (HY-13030) 与 Thalidomide (HY-14658) 衍生物通过 linker 产生的 PROTAC，能够在低纳摩尔浓度下诱导 BRD4 降解。
| Cas No.: |
1799711-21-9 |
| 名称: |
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| 别名: |
Dbet1,dBET-1 ,dBET 1 |
| SMILES: |
CC1=NN=C2[C@H](CC(NCCCCNC(COC3=CC=CC(C(N4C5C(NC(CC5)=O)=O)=O)=C3C4=O)=O)=O)N=C(C6=CC=C(Cl)C=C6)C7=C(SC(C)=C7C)N21 |
| 分子式: |
C38H37ClN8O7S |
| 分子量: |
785.3 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50= 0.14 μM, compare to IC50= 1.1 μM with JQ1). |
| Kinase Assay: |
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| Cell Assay: |
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| Animal Administration: |
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| References: |
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MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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