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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 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].
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 100 mg | 待询 | 待询 | |
| 500 mg | 待询 | 待询 |
| 产品描述 | 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]. |
| 体外活性 | 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]. |
| 分子量 | 1009.11 |
| 分子式 | C53H64N6O14 |
| CAS No. | 1799711-22-0 |
| Smiles | O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCC(NCCCCNC(CCC(NC4=CC([C@H](OC(=O)[C@H]5N(C(C(C(CC)(C)C)=O)=O)CCCC5)CCC6=CC(OC)=C(OC)C=C6)=CC=C4)=O)=O)=O |
| 密度 | 1.298 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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