HaloPROTAC-E
Based on 1 publication(s) in Google Scholar
HaloPROTAC-E is a SGK3/VPS34 HaloPROTAC degrader that degrades Halo-tagged SGK3 and VPS34, with a DC50 of 3-10 nM in HEK293 cells. HaloPROTAC-E induces ubiquitination and proteasomal degradation of target proteins. HaloPROTAC-E blocks downstream phosphorylation of SGK3 substrate NDRG1. HaloPROTAC-E is applicable for cancer research.
(Pink: SGK3 and Vps34 ligand (HY-W260045); Blue: VHL ligand (HY-100947); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.76%
- CAS. Nr.: 2365478-58-4
- Formel: C39H56ClN5O8S
- Molecular Weight:790.41
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) HaloPROTAC-E
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Biologische Aktivität
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SGK3 |
Vps34 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | DC50 |
3-10 nM
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Half-maximal degradation concentration of endogenous SGK3-Halo protein in HEK293 (SGK3-Halo CRISPR knock-in Clone 2) cells measured via immunoblot after 48 hours of incubation with HaloPROTAC-E.
Half-maximal degradation concentration of endogenous SGK3-Halo protein in HEK293 (SGK3-Halo CRISPR knock-in Clone 2) cells measured via immunoblot after 48 hours of incubation with HaloPROTAC-E.
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30978004 |
HaloPROTAC-E (1-1000 nM; 48 h) potently induces dose-dependent degradation of endogenous SGK3-Halo and Halo-VPS34 in HEK293 cells, with a DC50 of 3-10 nM[1].
HaloPROTAC-E (300 nM; 10-240 min) induces rapid, reversible degradation of endogenous SGK3-Halo (50% degradation within 20-30 min) and VPS34-Halo (50% degradation within 1-2 h) in HEK293 cells[1].
Degradation of endogenous SGK3-Halo and Halo-VPS34 in HEK293 cells induced by HaloPROTAC-E (300 nM; 6 h) depends on the Cullin2-VHL E3 ligase pathway and proteasomal activity[1].
HaloPROTAC-E (300 nM; 0-24 h) mediates the degradation of endogenous SGK3-Halo and Halo-VPS34 in HEK293 cells, thereby functionally blocking the downstream SGK3 signaling pathway and reducing the phosphorylation level of NDRG1 Thr346[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:1, 3, 10, 30, 100, 300, 500, 1000 nM
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Incubation Time:48 h
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Result:Induced dose-dependent degradation of endogenous SGK3-Halo and Halo-VPS34, with a DC50 of 3-10 nM and a maximum degradation of ~95% at 300 nM after 48 hour.
Chemical Information
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CAS. Nr. 2365478-58-4
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Appearance Oil
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Molecular Weight 790.41
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Formel C39H56ClN5O8S
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Color Colorless to light yellow
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SMILES
O=C(C1(CC1)C#N)N[C@@H](C(C)(C)C)C(N(C[C@@H]2O)[C@@H](C2)C(NCC(C=CC(C(SC=N3)=C3C)=C4)=C4OCCOCCOCCOCCCCCCCl)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (126.52 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (3.16 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:
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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.
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.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
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. 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 | 1.2652 mL | 6.3258 mL | 12.6517 mL | 31.6292 mL |
| 5 mM | 0.2530 mL | 1.2652 mL | 2.5303 mL | 6.3258 mL | |
| 10 mM | 0.1265 mL | 0.6326 mL | 1.2652 mL | 3.1629 mL | |
| 15 mM | 0.0843 mL | 0.4217 mL | 0.8434 mL | 2.1086 mL | |
| 20 mM | 0.0633 mL | 0.3163 mL | 0.6326 mL | 1.5815 mL | |
| 25 mM | 0.0506 mL | 0.2530 mL | 0.5061 mL | 1.2652 mL | |
| 30 mM | 0.0422 mL | 0.2109 mL | 0.4217 mL | 1.0543 mL | |
| 40 mM | 0.0316 mL | 0.1581 mL | 0.3163 mL | 0.7907 mL | |
| 50 mM | 0.0253 mL | 0.1265 mL | 0.2530 mL | 0.6326 mL | |
| 60 mM | 0.0211 mL | 0.1054 mL | 0.2109 mL | 0.5272 mL | |
| 80 mM | 0.0158 mL | 0.0791 mL | 0.1581 mL | 0.3954 mL | |
| 100 mM | 0.0127 mL | 0.0633 mL | 0.1265 mL | 0.3163 mL |
HaloPROTAC-E Related Classifications
HY-145752 Related Classifications
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