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Lenalidomide-I

Lenalidomide-I 是一种用于 E3 泛素连接酶的 cereblon (CRBN) 配体 Lenalidomide 的类似物,用于 CRBN 蛋白的募集。Lenalidomide-I 可通过 linker 连接到蛋白质配体上形成 PROTAC,如 PROTAC BET 降解剂 QCA570 。

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  • 货号: ajcx33146
  • CAS: 2207541-30-6
  • 别名: 3-(4-碘-1-氧代异吲哚啉-2-基)哌啶-2,6-二酮
  • 分子式: C13H11IN2O3
  • 分子量: 370.14
  • 纯度: >98%
  • 溶解度: DMSO : 25 mg/mL (67.54 mM; Need ultrasonic)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 [1].


Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].


[1]. Qin C, et, al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704.

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