Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
性状
Solid
IC50 & Target[1][2]
Cereblon
体外研究(In Vitro)
Lenalidomide-Br 可以通过接头与蛋白质的配体连接以形成 PROTAC。PROTAC 是泛素介导的促癌蛋白降解的诱导剂。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17.[2]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
溶解度数据
In Vitro: DMSO : 10 mg/mL (30.95 mM; ultrasonic and warming and heat to 60°C)配制储备液