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dFKBP-1

dFKBP-1
dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, the Thalidomide-based cereblon ligand, and a linker[1].
Catalog No. T18597Cas No. 1799711-22-0

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dFKBP-1

Catalog No. T18597Cas No. 1799711-22-0

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

Bioactivity
Description
dFKBP-1 is a potent PROTAC-based FKBP12 degrader incorporating the FKBP12 ligand SLF, 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].
Chemical Properties
Molecular Weight1009.11
FormulaC53H64N6O14
Cas No.1799711-22-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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