PROTAC SGK3 degrader-1
Based on 5 publication(s) in Google Scholar
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), a chemical probe, is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate).
(Pink: SGK3 ligand (HY-151009); Blue: VHL ligand (HY-120217); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 2381320-35-8
- Formula: C57H73FN10O11S2
- Molecular Weight:1157.38
-
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC SGK3 degrader-1
MoreAll PROTACs Isoforms
More
Biological Activity
|
VHL |
SGK3 |
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (0.3 μM, 4 weeks) in combination with GDC0941 inhibits cell growth in CAMA-1 or ZR-75-1 cells[1].
PROTAC SGK3 degrader-1 (0.1 μM, 48 h) reduces SGK3 levels by 65% without effecting SGK1, SGK2, or S6K1 in HEK293 cells[1].
PROTAC SGK3 degrader-1 (1-10 μM, 48 h) moderate reduces S6K1 levels in HEK293 cells[1].
PROTAC SGK3 degrader-1 ( >0.1 μM, 8 h) reduces NDRG1 phosphorylation in HEK293 cells, and induces degradation of SGK3, but not SGK1 or S6K in CAMA-1 and ZR-75-1cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:CAMA-1 or ZR-75-1 cells
-
Concentration:0.3 μM
-
Incubation Time:4 weeks
-
Result:Inhibited cell growth in combination with GDC0941.
-
Cell Line:HEK293 cells
-
Concentration:0.1 μM
-
Incubation Time:48 h
-
Result:Reduced SGK3 levels by 65% without effecting SGK1, SGK2, or S6K1.
Chemical Information
-
CAS No. 2381320-35-8
-
Appearance Solid
-
Molecular Weight 1157.38
-
Formula C57H73FN10O11S2
-
Color White to off-white
-
SMILES
FC1=C(C=C(C=C1)C)S(=O)(NC2=CC=C(C=C2)C3=NC4=C(C(OC[C@H]5CN(CCO5)CCCCCCOCCOCCOCC(N[C@H](C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)C(C)(C)C)=O)=N3)C=NN4)=O
-
Synonyms
SGK3-PROTAC1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Redox Biol
The SGK3-Catalase antioxidant signaling axis drives cervical cancer growth and therapy resistance. [Abstract]2023 Nov:67:102931. PMID: 37866161 -
Theranostics
2024 Jan 1;14(2):861-878. PMID: 38169564 -
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 -
Cell Cycle
Inhibition of SGK3 regulates hyperplastic scar development in rats through the MAPK/ERK signaling pathway. [Abstract]2026 Dec;25(1):1-16. PMID: 41674333 -
Solvent & Solubility
DMSO : ≥ 100 mg/mL (86.40 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)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.16 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Data Sheet (272 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
-
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 | 0.8640 mL | 4.3201 mL | 8.6402 mL | 21.6005 mL |
| 5 mM | 0.1728 mL | 0.8640 mL | 1.7280 mL | 4.3201 mL | |
| 10 mM | 0.0864 mL | 0.4320 mL | 0.8640 mL | 2.1601 mL | |
| 15 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4400 mL | |
| 20 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0800 mL | |
| 25 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8640 mL | |
| 30 mM | 0.0288 mL | 0.1440 mL | 0.2880 mL | 0.7200 mL | |
| 40 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5400 mL | |
| 50 mM | 0.0173 mL | 0.0864 mL | 0.1728 mL | 0.4320 mL | |
| 60 mM | 0.0144 mL | 0.0720 mL | 0.1440 mL | 0.3600 mL | |
| 80 mM | 0.0108 mL | 0.0540 mL | 0.1080 mL | 0.2700 mL |
PROTAC SGK3 degrader-1 Related Classifications
HY-125878 Related Classifications
Powered by Bioz