dBRD9 是一种 PROTAC,能选择性的降解 BRD9。dBRD9 改进了溴域接合剖面,降低了整个 BET 家族的结合活性。
生物活性
dBRD9 is a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.
性状
Solid
IC50 & Target[1][2]
BRD9
体外研究(In Vitro)
dBRD9 (0.5-5000 nM;4 h) 在 MOLM-13 细胞中以浓度依赖性方式降低 BRD9 的表达,对肌动蛋白、BRD4、BRD7 表达无显著影响。dBRD9 (100 nM;2 h) 在 MOLM-13 细胞中对 BRD9 具有选择性。dBRD9 (7 d) 对 EOL-1 和 MOML-13 细胞系有抗增殖作用。 has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Remillard D, et al. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angew Chem Int Ed Engl. 2017 May 15;56(21):5738-5743.
溶解度数据
In Vitro: DMSO : 100 mg/mL (127.58 mM; Need ultrasonic)配制储备液