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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Cereblon FKBP
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
dFKBP-1
CAS number：1799711-22-0 molecular formula：C53H64N6O14
overview
compound introduction
Specs
| Chinese alias | 去氨KBP-1 | ||
| English alias | DTXSID901098019 | dFKBP-1 | MS-31862 | 2-Piperidinecarboxylic acid, 1-(3,3-dimethyl-1,2-dioxopentyl)-, (1R)-3-(3,4-dimethoxyphenyl)-1-[3-[[4-[[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]amino]-1,4-dio | ||
| CAS number | 1799711-22-0 | molecular formula | C53H64N6O14 |
| molecular weight | 1009.11 g/mol | Exact mass | ≥95% |
| PSA | 262.000 Ų | logp | 4.200 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
