Nur77 modulator 1
Based on 1 Customer Validation
Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
For research use only. We do not sell to patients.
- Purity: 98.16%
- CAS No.: 2469975-55-9
- Formula: C28H25N5O2S
- Molecular Weight:495.60
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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All Nuclear Hormone Receptor 4A/NR4A Isoforms
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Biological Activity
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Nur77/NR4A1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
0.6 μM
Compound: 10g
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Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| L02 | IC50 |
>20 μM
Compound: 10g
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| QGY-7703 | IC50 |
0.89 μM
Compound: 10g
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Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
| SMMC-7721 | IC50 |
1.4 μM
Compound: 10g
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Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32717483] |
Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line)[1].
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner[1].
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis[1].
Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
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Concentration:0-20 μM.
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Incubation Time:12-24 hours.
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Result:Exhibited IC50 values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively.
Reduced the viability in a time-dependent manner.
Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mouse hepatoma HepG2 xenograft[1].
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Dosage:10 and 20 mg/kg/day.
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Administration:IP, once every day for 15 days.
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Result:Lead to substantial suppression of tumor growth.
The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively.
Exhibited almost no influence on the body weight of experimental mice.
Chemical Information
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CAS No. 2469975-55-9
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Appearance Solid
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Molecular Weight 495.60
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Formula C28H25N5O2S
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Color White to yellow
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SMILES
CC1=NC2=C(OC)C=CC=C2C(NC3=CC4=C(NC(C(N/N=C/C5=CC=C(SC)C=C5)=O)=C4)C=C3)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL (252.22 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 (protect from light). 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 (protect from light). 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: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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 (protect from light). 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 | 2.0178 mL | 10.0888 mL | 20.1776 mL | 50.4439 mL |
| 5 mM | 0.4036 mL | 2.0178 mL | 4.0355 mL | 10.0888 mL | |
| 10 mM | 0.2018 mL | 1.0089 mL | 2.0178 mL | 5.0444 mL | |
| 15 mM | 0.1345 mL | 0.6726 mL | 1.3452 mL | 3.3629 mL | |
| 20 mM | 0.1009 mL | 0.5044 mL | 1.0089 mL | 2.5222 mL | |
| 25 mM | 0.0807 mL | 0.4036 mL | 0.8071 mL | 2.0178 mL | |
| 30 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6815 mL | |
| 40 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2611 mL | |
| 50 mM | 0.0404 mL | 0.2018 mL | 0.4036 mL | 1.0089 mL | |
| 60 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8407 mL | |
| 80 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
| 100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL |
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