PROTAC MEK1 Degrader-1
Based on 1 Customer Validation
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells.
(Pink: MEK1 ligand (HY-175585); Blue: VHL ligand (HY-112078); Black: linker (HY-33366)).
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 2671004-41-2
- Formula: C53H66FIN8O11S2
- Molecular Weight:1201.17
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Storage:Powder -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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| SU-DHL-1 | GI50 |
2400 nM
Compound: 4
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Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
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[PMID: 33284613] |
PROTAC MEK1 Degrader-1 (Compound 3) (10 μM-100 pM; 12 h) occurs degradation at the two highest concentrations of 1 μM and 10 μM, whereas lower concentrations lead to an increase of MEK1 and ERK1/2 expression[1]. PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 12 h) strongly suppresses in regulation of secretion of cytokines, such as IL6[1]. PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-72 h) shows an antiproliferative activity against A375 cells [1]. PROTAC MEK1 Degrader-1 (Compound 3) (10 μM; 0-20 h) can significantly degrade MEK1 and ERK1/2 after 5 h, and completely inhibit from 8 hours later[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 cells
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Concentration:10 μM
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Incubation Time:0 h, 20 h, 40 h, 60 h, 80h
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Result:Had a strong inhibitory effect on cell growth
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Cell Line:A375 cells
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Concentration:10 μM
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Incubation Time:16 h
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Result:It degraded MEK and inhibited phosphorylation of ERK1/2.
Chemical Information
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CAS No. 2671004-41-2
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Appearance Solid
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Molecular Weight 1201.17
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Formula C53H66FIN8O11S2
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Color White to off-white
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SMILES
O=S(NC(C=C(C(N1C)=O)C)=C1NC2=C(C=C(C=C2)I)F)(C3=CC=C(C=C3)CCC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (83.25 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.
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 (2.08 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.08 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 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.
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.
Purity & Documentation
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Data Sheet (272 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. 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 | 0.8325 mL | 4.1626 mL | 8.3252 mL | 20.8130 mL |
| 5 mM | 0.1665 mL | 0.8325 mL | 1.6650 mL | 4.1626 mL | |
| 10 mM | 0.0833 mL | 0.4163 mL | 0.8325 mL | 2.0813 mL | |
| 15 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3875 mL | |
| 20 mM | 0.0416 mL | 0.2081 mL | 0.4163 mL | 1.0407 mL | |
| 25 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8325 mL | |
| 30 mM | 0.0278 mL | 0.1388 mL | 0.2775 mL | 0.6938 mL | |
| 40 mM | 0.0208 mL | 0.1041 mL | 0.2081 mL | 0.5203 mL | |
| 50 mM | 0.0167 mL | 0.0833 mL | 0.1665 mL | 0.4163 mL | |
| 60 mM | 0.0139 mL | 0.0694 mL | 0.1388 mL | 0.3469 mL | |
| 80 mM | 0.0104 mL | 0.0520 mL | 0.1041 mL | 0.2602 mL |
PROTAC MEK1 Degrader-1 Related Classifications
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