NR-V04
Based on 1 Customer Validation
NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8+ T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer.
(Pink: Nur77/NR4A1 ligand (HY-13067); Blue: VHL ligand (HY-112078); Black: linker (HY-130524)).
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 2766608-52-8
- Formula: C62H87N5O11S
- Molecular Weight:1110.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Immunology/Inflammation Compound Library
HY-L007
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Anti-Cancer Compound Library
HY-L025
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Transcription Factor-Targeted Library
HY-L090
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Anti-Colorectal Cancer Compound Library
HY-L103
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Nuclear Receptor Compound Library
HY-L126
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PROTAC Library
HY-L151
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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VHL |
Nur77/NR4A1 |
NR-V04 (250 nM; 16 h) potently reduces NR4A1 protein levels in CHL-1 human melanoma cells[1].
NR-V04 (125-1000 nM; 16 h) induces dose-dependent NR4A1 degradation in CHL-1 (DC50 = 228.5 nM) and A375 (DC50 = 518.8 nM) human melanoma cells without affecting NR4A2 or NR4A3 levels, while accumulating VHL protein[1].
NR-V04 (500-1000 nM; 16 h) reduces NR4A1 protein levels in WM164, M229 human melanoma cells, and SM1, SW1 mouse melanoma cells[1].
NR-V04 (500 nM; 4-48 h) induces time-dependent NR4A1 degradation in CHL-1 human melanoma cells, with an initial protein induction at 4 h and efficient degradation occurring between 8 and 48 h[1].
NR-V04 (500 nM; 16 h) induces ternary complex formation between NR4A1 and VHL in HEK293T cells overexpressing Flag-NR4A1[1].
NR-V04 (500 nM) significantly reduces the percentage of exhausted CD8+ T cells in human PBMC-derived CD8+ T cell cultures[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHL-1, A375 human melanoma cells
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Concentration:125, 250, 500, 1000 nM
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Incubation Time:16 h
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Result:Induced a dose-dependent decrease of NR4A1 protein with a DC50 of 228.5 nM in CHL-1 cells and a DC50 of 518.8 nM in A375 cells.
Led to accumulation of VHL protein in both cell lines.
Selectively reduced NR4A1 protein levels.
Spared NR4A2 and NR4A3 protein levels in both cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice with B16F10, MC38 and Yumm1.7 (7-9 weeks)[1]
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Dosage:1.8 mg/kg
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Administration:I.p.; at day 7
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Result:Inhibited tumor growth.
Increased B cell percentage in the TME, but not in spleen and blood.
Induces tumor-infiltrating B cells and effector memory CD8+ T cells.
Reduced monocytic myeloid-derived suppressor cells in tumor microenvironments.
Chemical Information
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CAS No. 2766608-52-8
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Appearance Solid
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Molecular Weight 1110.45
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Formula C62H87N5O11S
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Color Orange to red
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SMILES
C[C@@]12[C@]([C@@]3([H])[C@@](CC1)(CC[C@](C)(C3)C(NCCOCCOCCOCCOCC(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(N=CS6)C)C=C5)C)=O)=O)=O)=O)C)(CC[C@@]7(C2=CC=C8C7=CC(C(O)=C8C)=O)C)C
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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 (90.05 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 (2.25 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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 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 |
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| DMSO | 1 mM | 0.9005 mL | 4.5027 mL | 9.0054 mL | 22.5134 mL |
| 5 mM | 0.1801 mL | 0.9005 mL | 1.8011 mL | 4.5027 mL | |
| 10 mM | 0.0901 mL | 0.4503 mL | 0.9005 mL | 2.2513 mL | |
| 15 mM | 0.0600 mL | 0.3002 mL | 0.6004 mL | 1.5009 mL | |
| 20 mM | 0.0450 mL | 0.2251 mL | 0.4503 mL | 1.1257 mL | |
| 25 mM | 0.0360 mL | 0.1801 mL | 0.3602 mL | 0.9005 mL | |
| 30 mM | 0.0300 mL | 0.1501 mL | 0.3002 mL | 0.7504 mL | |
| 40 mM | 0.0225 mL | 0.1126 mL | 0.2251 mL | 0.5628 mL | |
| 50 mM | 0.0180 mL | 0.0901 mL | 0.1801 mL | 0.4503 mL | |
| 60 mM | 0.0150 mL | 0.0750 mL | 0.1501 mL | 0.3752 mL | |
| 80 mM | 0.0113 mL | 0.0563 mL | 0.1126 mL | 0.2814 mL |
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