ligand
C5 Lenalidomide
品質等級
化驗
≥95%
形狀
powder
儲存溫度
2-8°C
SMILES 字串
O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(COCC(F)(F)COCCCCN4CCNCC4)=O)=CC=C31.Cl
應用
Protein degrader building block C5 Lenalidomide-difluoroPEG1-C4-piperazine Hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a fluorinated linker with both hydrophobic and hydrophilic moieties, and a pendant amine for reactivity with a carboxylic acid on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Targeted Protein Degradation
Targeted Protein Degradation
訊號詞
Warning
危險聲明
危險分類
Repr. 2 - STOT RE 2
標靶器官
Blood
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
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