dFKBP-1
Based on 1 publication(s) in Google Scholar
dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker.
(Pink: FKBP12 ligand (HY-114872); Blue: E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.00%
- CAS No.: 1799711-22-0
- Formula: C53H64N6O14
- Molecular Weight:1009.11
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) dFKBP-1
MoreAll PROTACs Isoforms
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Biological Activity
|
Cereblon |
FKBP12 |
FKBP |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1799711-22-0
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Appearance Solid
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Molecular Weight 1009.11
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Formula C53H64N6O14
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Color Off-white to light yellow
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SMILES
O=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@H](C2=CC=CC(NC(CCC(NCCCCNC(COC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)=O)=O)=O)=C2)CCC6=CC=C(OC)C(OC)=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Jun 26;15(1):5409. PMID: 38926334
Solvent & Solubility
DMSO : ≥ 100 mg/mL (99.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9910 mL | 4.9549 mL | 9.9097 mL | 24.7743 mL |
| 5 mM | 0.1982 mL | 0.9910 mL | 1.9819 mL | 4.9549 mL | |
| 10 mM | 0.0991 mL | 0.4955 mL | 0.9910 mL | 2.4774 mL | |
| 15 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6516 mL | |
| 20 mM | 0.0495 mL | 0.2477 mL | 0.4955 mL | 1.2387 mL | |
| 25 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9910 mL | |
| 30 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 40 mM | 0.0248 mL | 0.1239 mL | 0.2477 mL | 0.6194 mL | |
| 50 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL | |
| 60 mM | 0.0165 mL | 0.0826 mL | 0.1652 mL | 0.4129 mL | |
| 80 mM | 0.0124 mL | 0.0619 mL | 0.1239 mL | 0.3097 mL |