MG-HuR2
Based on 1 publication(s) in Google Scholar
MG-HuR2 is a molecular glue degrader targeting HuR (ELAVL1) with a Kd of 0.2018 μM. MG-HuR2 recruits the E3 ubiquitin ligase RNF126 and induces proteasome-dependent degradation of HuR. MG-HuR2 exhibits a unique biphasic degradation profile. MG-HuR2 reduces the expression of HuR and its downstream targets Bcl2/FOXQ1, inhibits breast cancer cell proliferation, enhances cytotoxicity and apoptosis (apoptosis), and suppresses the growth of 3D breast cancer tumor spheres. MG-HuR2 can be used in studies related to breast cancer and HuR-targeted protein degradation.
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- Pureté: 98.70%
- CAS No.: 3098773-64-6
- Formule: C22H20N2O5
- Masse moléculaire:392.40
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MG-HuR2
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Activité biologique
Description
IC50 & Target
[1]|
HuR 0.2018 μM (Kd) |
In Vitro
MG-HuR2 binds tightly to purified HuR RRM1/2 protein in fluorescence polarization displacement assays, with a Kd value of 0.2018 μM[1].
MG-HuR2 (10 μM; 24 h) effectively degrades GFP-tagged HuR in HEK-293 cells[1].
MG-HuR2 binds to two distinct RNA-binding pockets on HuR. Calculations of binding energy via MM-GBSA show that its affinity for the P1 pocket (-46.76 kcal/mol) is higher than that for the P2 pocket (-39.04 kcal/mol)[1].
MG-HuR2 (1 nM-10 μM; 24 h) induces proteasome-dependent biphasic degradation of HuR in MCF-7 and MDA-MB-231 breast cancer cells. After 24 h, HuR expression is reduced by up to 85% at 10 nM and up to 80% at 10 μM[1].
MG-HuR2 (1-100 nM) reduces the expression of HuR-associated Bcl2 and FOXQ1 mRNA in MCF-7 cells; Bcl2 mRNA rebounds at 1 μM, which is consistent with the hook effect of MG-HuR2[1].
MG-HuR2 (10 nM; 24 h) reduces Bcl2 protein expression in MCF-7 and MDA-MB-231 cells by 88% and 45%, respectively[1].
MG-HuR2 (10 nM or 10 μM) reduces the viability of MCF-7 breast cancer cells, whereas it causes no significant cytotoxicity or change in cell viability in non-tumorigenic mammary epithelial MCF-10A cells[1].
MG-HuR2 (0.1 nM-100 μM; 24 or 48 h) significantly inhibits the proliferation of MCF-7 and MDA-MB-231 breast cancer cells, with a more pronounced inhibitory effect at 48 h[1].
MG-HuR2 (10 nM) inhibits the growth of tumorspheres starting from day 2 and continuously reduces the surface area of tumorspheres during the subsequent observation period in 3D breast cancer tumorsphere models of MCF-7 and MDA-MB-231[1].
MG-HuR2 (1 nM-1 μM; 24 or 48 h) enhances caspase-3/7 activity in MCF-7 cells and significantly induces apoptosis at 10 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 breast cancer cells, MDA-MB-231 breast cancer cells
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Concentration:10 nM-10 μM
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Incubation Time:24 h
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Result:Reduced HuR by 85% and 56% at 10 nM and by 80% and 59% at 10 μM in MCF-7 and MDA-MB-231 cells, respectively, with a biphasic degradation profile.
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Cell Line:MCF-7 breast cancer cells
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Concentration:MG-HuR2 10 μM; MG132 or bortezomib 1 μM
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Incubation Time:5 h
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Result:Proteasome inhibition blocked HuR degradation, supporting a proteasome-dependent degradation mechanism.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1 nM-1 μM
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Incubation Time:24 h
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Result:Reduced Bcl2 mRNA at low nanomolar concentrations, with rebound at 1 μM consistent with the hook effect.
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Cell Line:MCF-7 breast cancer cells, MDA-MB-231 breast cancer cells
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Concentration:0.1 nM-100 μM
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Incubation Time:24 h; 48 h
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Result:Significantly reduced cell proliferation, with stronger inhibition at 48 h.
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Cell Line:MCF-7 breast cancer cells
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Concentration:1 nM-1 μM
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Incubation Time:24 h; 48 h
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Result:Increased caspase-3/7-dependent apoptosis, with a significant increase at 10 nM.
Chemical Information
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CAS No. 3098773-64-6
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Appearance Solid
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Masse moléculaire 392.40
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Formule C22H20N2O5
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Color Light yellow to orange
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SMILES
CCOC(C1=CC2=CC(NC(/C=C/C(C3=CC=C(C=C3)OC)=O)=O)=CC=C2N1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (254.84 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)
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.
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.
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.5484 mL | 12.7421 mL | 25.4842 mL | 63.7105 mL |
| 5 mM | 0.5097 mL | 2.5484 mL | 5.0968 mL | 12.7421 mL | |
| 10 mM | 0.2548 mL | 1.2742 mL | 2.5484 mL | 6.3711 mL | |
| 15 mM | 0.1699 mL | 0.8495 mL | 1.6989 mL | 4.2474 mL | |
| 20 mM | 0.1274 mL | 0.6371 mL | 1.2742 mL | 3.1855 mL | |
| 25 mM | 0.1019 mL | 0.5097 mL | 1.0194 mL | 2.5484 mL | |
| 30 mM | 0.0849 mL | 0.4247 mL | 0.8495 mL | 2.1237 mL | |
| 40 mM | 0.0637 mL | 0.3186 mL | 0.6371 mL | 1.5928 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5097 mL | 1.2742 mL | |
| 60 mM | 0.0425 mL | 0.2124 mL | 0.4247 mL | 1.0618 mL | |
| 80 mM | 0.0319 mL | 0.1593 mL | 0.3186 mL | 0.7964 mL | |
| 100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6371 mL |
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