(R,S,R)-ML334
Based on 1 Customer Validation
(R,S,R)-ML334 is the isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
For research use only. We do not sell to patients.
- Purity: 98.57%
- CAS No.: 1432065-33-2
- Formula: C26H26N2O5
- Molecular Weight:446.50
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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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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
>100 μM
Compound: (RSR)-5, isomer B
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Inhibition of Keap1-Nrf2 interaction in human HepG2 cells expressing ARE-bla assessed as activation of antioxidant response element by beta-lactamase reporter assay
Inhibition of Keap1-Nrf2 interaction in human HepG2 cells expressing ARE-bla assessed as activation of antioxidant response element by beta-lactamase reporter assay
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[PMID: 23562243] |
| U2OS | EC50 |
>100 μM
Compound: (RSR)-5, isomer B
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Inhibition of Keap1-Nrf2 interaction in human U2OS cells assessed as Nrf2 nuclear translocation by beta-lactamase reporter assay
Inhibition of Keap1-Nrf2 interaction in human U2OS cells assessed as Nrf2 nuclear translocation by beta-lactamase reporter assay
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[PMID: 23562243] |
Chemical Information
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CAS No. 1432065-33-2
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Appearance Solid
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Molecular Weight 446.50
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Formula C26H26N2O5
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Color White to off-white
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SMILES
O=C([C@H]1[C@@H](C(N2[C@@H](CN(C(C3=C4C=CC=C3)=O)C4=O)C5=C(C=CC=C5)CC2)=O)CCCC1)O
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Synonyms
(R,S,R)-LH601A
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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 (223.96 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.20 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
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.
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 (278 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
[1]. Wen X, et al. Activation of NRF2 Signaling in HEK293 Cells by a First-in-Class Direct KEAP1-NRF2 Inhibitor. J Biochem Mol Toxicol. 2015 Jun;29(6):261-6. [Content Brief]
[2]. Hu L, et al. Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. Bioorg Med Chem Lett. 2013 May 15;23(10):3039-43. [Content Brief]
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 | 2.2396 mL | 11.1982 mL | 22.3964 mL | 55.9910 mL |
| 5 mM | 0.4479 mL | 2.2396 mL | 4.4793 mL | 11.1982 mL | |
| 10 mM | 0.2240 mL | 1.1198 mL | 2.2396 mL | 5.5991 mL | |
| 15 mM | 0.1493 mL | 0.7465 mL | 1.4931 mL | 3.7327 mL | |
| 20 mM | 0.1120 mL | 0.5599 mL | 1.1198 mL | 2.7996 mL | |
| 25 mM | 0.0896 mL | 0.4479 mL | 0.8959 mL | 2.2396 mL | |
| 30 mM | 0.0747 mL | 0.3733 mL | 0.7465 mL | 1.8664 mL | |
| 40 mM | 0.0560 mL | 0.2800 mL | 0.5599 mL | 1.3998 mL | |
| 50 mM | 0.0448 mL | 0.2240 mL | 0.4479 mL | 1.1198 mL | |
| 60 mM | 0.0373 mL | 0.1866 mL | 0.3733 mL | 0.9332 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2800 mL | 0.6999 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2240 mL | 0.5599 mL |
(R,S,R)-ML334 Related Classifications
HY-110258B Related Classifications
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