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dFKBP-1

Catalog No. T18597 CAS 1799711-22-0

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].

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dFKBP-1, CAS 1799711-22-0

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Biological Description

Chemical Properties

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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].

In vitro

dFKBP-1 significantly reduces FKBP12 levels in MV4;11 cells, achieving over an 80% decrease at 0.1 μM and a 50% decrease at 0.01 μM. Similarly to dBET1, dFKBP-1's effect on FKBP12 destabilization can be reversed by pre-treatment with Carfilzomib, MLN4924, free SLF, or free Thalidomide. The mechanism of Cereblon (CRBN)-dependent degradation was confirmed using established isogenic 293FT cell lines, both wild-type (293FT-WT) and CRBN-deficient (293FT-CRBN?/?). dFKBP-1 treatment led to a potent and dose-dependent decrease in FKBP12 in 293FT-WT cells, with no impact observed on 293FT-CRBN?/? cells[1].

Molecular Weight	1009.11
Formula	C53H64N6O14
CAS No.	1799711-22-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

dFKBP-1 1799711-22-0 Others dFKBP1 dFKBP 1 inhibitor inhibit

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