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dFKBP-1
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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].
dFKBP-1
😃Good
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
Chemical Properties
| 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]. |
| Molecular Weight | 1009.11 |
| Formula | C53H64N6O14 |
| Cas No. | 1799711-22-0 |
| Relative Density. | 1.298 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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