PROTAC FKBP Degrader-3
Based on 1 publication(s) in Google Scholar
PROTAC FKBP Degrader-3 is a selective FKBP PROTAC degrader with an IC50 of 1.8 nM. PROTAC FKBP Degrader-3 targets and degrades the FKBP protein by recruiting the VHL E3 ligase, and this degradation process is primarily mediated by K11 and K48 ubiquitin chain linkages. PROTAC FKBP Degrader-3 can be applied in cancer research.
(Pink: FKBP ligand (HY-114434); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).
For research use only. We do not sell to patients.
- Purity: 99.14%
- CAS No.: 2079056-43-0
- Formula: C68H90N6O17S
- Molecular Weight:1295.54
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC FKBP Degrader-3
MoreAll PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
VHL |
In Vitro
PROTAC FKBP Degrader-3 (Compound 10) (250 nM; 1-3 h) recruits endogenous VHL to induce the formation of K11- and K48-linked polyubiquitin chains on EGFP-FKBP in Flp-In TREx 293 cells[1].
PROTAC FKBP Degrader-3 (25-500 nM; 24 h) induces the degradation of the target protein (EGFP-FKBP) in Flp-In T-REx 293 cells stably expressing EGFP-FKBP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Flp-In T-REx 293 cells stably expressing EGFP-FKBP
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Concentration:250 nM
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Incubation Time:1 h, 2 h, 3 h
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Result:Significantly induced the polyubiquitination of the reporter protein (EGFP-FKBP), and this effect reached a steady state that was maintained over the following 2 hours.
Chemical Information
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CAS No. 2079056-43-0
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Appearance Solid
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Molecular Weight 1295.54
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Formula C68H90N6O17S
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Color Off-white to light yellow
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SMILES
CC[C@H](C(N1[C@H](C(O[C@H](CCC2=CC=C(OC)C(OC)=C2)C3=CC=CC(OCC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=C3)=O)CCCC1)=O)C7=CC(OC)=C(OC)C(OC)=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°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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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (19.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (3.86 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
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| DMSO | 1 mM | 0.7719 mL | 3.8594 mL | 7.7188 mL | 19.2970 mL |
| 5 mM | 0.1544 mL | 0.7719 mL | 1.5438 mL | 3.8594 mL | |
| 10 mM | 0.0772 mL | 0.3859 mL | 0.7719 mL | 1.9297 mL | |
| 15 mM | 0.0515 mL | 0.2573 mL | 0.5146 mL | 1.2865 mL |
PROTAC FKBP Degrader-3 Related Classifications
HY-135345 Related Classifications
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