1799711-22-0
1799711-22-0 structure
- Name: dFKBP-1
- Chemical Name: dFKBP-1
- CAS Number: 1799711-22-0
- Molecular Formula: C53H64N6O14
- Molecular Weight: 1009.11
- Catalog: Signaling Pathways PROTAC PROTAC
- Create Date: 2020-04-07 21:36:58
- Modify Date: 2024-01-08 17:01:18
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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].
| Name | dFKBP-1 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
Cereblon FKBP |
| In Vitro | 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]. |
| References |
| Molecular Formula | C53H64N6O14 |
|---|---|
| Molecular Weight | 1009.11 |