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- FKBP (FK506-binding protein)
- dFKBP-1
dFKBP-1
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。
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包装价格促销价数量
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1mg￥5937.004750.00- +
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5mg￥16025.0012820.00- +
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10mg￥25650.0020520.00- +
- 货号: ajcx29280
- CAS: 1799711-22-0
- 别名:
- 分子式: C53H64N6O14
- 分子量: 1009.11
- 纯度: ＞98%
- 溶解度: DMSO: 100 mg/mL (99.10 mM)
- 储存: 4°C, stored under nitroge
- 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.
