U7D-1
Based on 1 Customer Validation
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells.
(Pink: USP7 ligand (HY-49319); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 3094177-94-0
- Formula: C53H65N9O7
- Molecular Weight:940.14
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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
All PROTACs Isoforms
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Biological Activity
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USP7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JeKo-1 | IC50 |
1034 nM
Compound: 26; U7D-1
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Antiproliferative activity against human JeKo-1 cells harbouring p53 mutant
Antiproliferative activity against human JeKo-1 cells harbouring p53 mutant
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[PMID: 36306471] |
U7D-1 (0-1 μM, 0-24 h) induced USP7 degradation in RS4;11 cell, reducing the USP7 protein level by 83.2% at 1 μM[1].
U7D-1 (0-20 μM, 3 days) shows anti-proliferative activity in p53 wild-type cell lines, and maintains potent cell growth inhibition in p53 mutant cancer cells[1].
U7D-1 (1 μM, 0-24 h) upregulates the level of p53 and p21 proteins in a time-dependent manner, and induces cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner[1].
U7D-1 (1 μM, 24 h) up-regulates the expression of apoptotic related genes and down-regulates the expression of E2F related genes in Jeko-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11 cells
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Concentration:0, 5, 20, 50, 100, and 500 nM
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Incubation Time:24 h
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Result:Induced USP7 degradation in RS4;11 cell in a dose dependent manner, with a DC50 (half-maximal degradation) value of 33 nM.
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Cell Line:p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines); p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM)
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Concentration:0-20 μM
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Incubation Time:3 days
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Result:Showed antiproliferative activity in p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines), and p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM), with IC50 values for 3 days of 79.4, 227.0, 830.3, 1367.2, 4948.0, 1034.9, 1175.3, 1860.6, 6077.6, 9078.0, and 10675.0, respectively. Had an antiproliferative activity with an IC50 value of 53.5 nM in Jeko-1 cells for 7 days but exhibited a 13-fold loss in antiproliferative activity with an IC50 value of 727 nM in Jeko-1 CRBN KO cells.
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Cell Line:RS4;11 cells, Jeko-1 and Mino cell
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Concentration:1 μM
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Incubation Time:0, 2, 4, 6, 8, 10, 12, 20, 24, 36, 48, 60, and 72 h
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Result:USP7 degradation in RS4;11 cells induced by U7D-1 started after 4 h of exposure and more effective degradation was observed after 8 h of exposure. Up-regulated the level of p53 and p21 proteins in RS4;11 cells in a time-dependent manner. Had no effect on the level of p53 protein in p53-mutant cell lines. Induced cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner.
Chemical Information
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CAS No. 3094177-94-0
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Appearance Solid
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Molecular Weight 940.14
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Formula C53H65N9O7
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Color White to light yellow
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCCCCCCNCC4=CC=C(C5=C(C6=NN5C)N=CN(CC7(O)CCN(C(C[C@H](C8=CC=CC=C8)C)=O)CC7)C6=O)C=C4)=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 (106.37 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 (2.66 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 (2.66 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 | 1.0637 mL | 5.3184 mL | 10.6367 mL | 26.5918 mL |
| 5 mM | 0.2127 mL | 1.0637 mL | 2.1273 mL | 5.3184 mL | |
| 10 mM | 0.1064 mL | 0.5318 mL | 1.0637 mL | 2.6592 mL | |
| 15 mM | 0.0709 mL | 0.3546 mL | 0.7091 mL | 1.7728 mL | |
| 20 mM | 0.0532 mL | 0.2659 mL | 0.5318 mL | 1.3296 mL | |
| 25 mM | 0.0425 mL | 0.2127 mL | 0.4255 mL | 1.0637 mL | |
| 30 mM | 0.0355 mL | 0.1773 mL | 0.3546 mL | 0.8864 mL | |
| 40 mM | 0.0266 mL | 0.1330 mL | 0.2659 mL | 0.6648 mL | |
| 50 mM | 0.0213 mL | 0.1064 mL | 0.2127 mL | 0.5318 mL | |
| 60 mM | 0.0177 mL | 0.0886 mL | 0.1773 mL | 0.4432 mL | |
| 80 mM | 0.0133 mL | 0.0665 mL | 0.1330 mL | 0.3324 mL | |
| 100 mM | 0.0106 mL | 0.0532 mL | 0.1064 mL | 0.2659 mL |
U7D-1 Related Classifications
HY-148369 Related Classifications
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