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- Epigenetic Reader Domain
- ARV-825
ARV-825
A BRD4 inhibitor that drives BRD4 degradation
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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5mg￥1386.001108.00- +
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10mg￥2394.001915.00- +
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50mg￥6682.005345.00- +
- 货号: ajci22318
- CAS: 1818885-28-7
- 别名:
- 分子式: C46H47ClN8O9S
- 分子量: 923.43
- 纯度: ＞98%
- 溶解度: DMSO : ≥ 50 mg/mL (54.15 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 uM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors[1].
参考文献:
[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.
Protocol
Kinase experiment: | Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX[1]. |
参考文献: [1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. | |
