dFKBP-1 是一种基于 PROTAC 的有效的 FKBP12 降解剂。dFKBP-1 包含 FKBP12 配体 SLF，基于 Thalidomide 的 cereblon 配体和一个 linker。
货号:ajcx29280
CAS:1799711-22-0
分子式:C53H64N6O14
分子量：1009.11
溶解度:DMSO: 100 mg/mL (99.10 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1].

dFKBP-1 potently decreases FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM. As with dBET1, destabilization of FKBP12 by dFKBP-1 is rescued by pre-treatment with Carfilzomib, MLN4924, free SLF or free Thalidomide. Cereblon (CRBN)-dependent degradation is established using previously published isogenic 293FT cell lines which are wild-type (293FT-WT) or deficient (293FT-CRBN-/-) for CRBN. Treatment of 293FT-WT cells with dFKBP-1 induces potent, dose-dependent degradation of FKBP12, whereas 293FT-CRBN-/- are unaffected[1].

[1]. Winter GE, et al. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015 Jun 19;348(6241):1376-81.