ZM223
ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.
For research use only. We do not sell to patients.
- CAS No.: 2031177-48-5
- Formula: C23H17F3N4O2S2
- Molecular Weight:502.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
Biological Activity
NEDD8 activating enzyme (NAE)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
41.23 μM
Compound: ZM223
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Antiproliferative activity against human A549 cells by CCK8 assay
Antiproliferative activity against human A549 cells by CCK8 assay
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[PMID: 38320715] |
| HCT-116 | IC50 |
0.1 μM
Compound: 7g; ZM223
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Antitumor activity against human HCT116 cells after 72 hrs by MTT assay
Antitumor activity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 28388520] |
| KYSE-30 | IC50 |
17.38 μM
Compound: ZM223
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Antiproliferative activity against human KYSE-30 cells by CCK8 assay
Antiproliferative activity against human KYSE-30 cells by CCK8 assay
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[PMID: 38320715] |
| MCF7 | IC50 |
>100 μM
Compound: ZM223
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Antiproliferative activity against human MCF7 cells by CCK8 assay
Antiproliferative activity against human MCF7 cells by CCK8 assay
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[PMID: 38320715] |
| MGC-803 | IC50 |
4.91 μM
Compound: ZM223
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Antiproliferative activity against human MGC-803 cells by CCK8 assay
Antiproliferative activity against human MGC-803 cells by CCK8 assay
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[PMID: 38320715] |
| U2OS | IC50 |
1.22 μM
Compound: 7g; ZM223
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Antitumor activity against human U2OS cells after 72 hrs by MTT assay
Antitumor activity against human U2OS cells after 72 hrs by MTT assay
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[PMID: 28388520] |
ZM223 (0.1-1 μM; 4 hours) inhibits both HCT-116 and U-2OS cancer cells with IC50s of 100 and 122 nM, respectively[1]. ZM223 (0.1-1 μM; 4 hours) causes a dose-response decrease in the level of NEDD8 and accumulation of the UBC12 protein, indicating the decrease of the subsequent NEDD8-UBC12 complex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 colon cancer cells and U-2OS osteosarcoma cells
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Concentration:0.1 μM, 1 μM
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Incubation Time:4 hours
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Result:Inhibited both HCT-116 and U-2OS cancer cells.
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Cell Line:HCT116 colon cancer cells
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Concentration:0.1 μM, 1 μM
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Incubation Time:4 hours
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Result:Caused a decrease in the level of NEDD8 and an increase in the downstream UBC12 protein.
Chemical Information
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CAS No. 2031177-48-5
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Molecular Weight 502.53
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Formula C23H17F3N4O2S2
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SMILES
O=C(C1=CC=C(C(F)(F)F)C=C1)NC2=NC3=CC=C(NC(CSC4=CC=C(N)C=C4)=O)C=C3S2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
DMSO : 83.33 mg/mL (165.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.08 mg/mL (4.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9899 mL | 9.9497 mL | 19.8993 mL | 49.7483 mL |
| 5 mM | 0.3980 mL | 1.9899 mL | 3.9799 mL | 9.9497 mL | |
| 10 mM | 0.1990 mL | 0.9950 mL | 1.9899 mL | 4.9748 mL | |
| 15 mM | 0.1327 mL | 0.6633 mL | 1.3266 mL | 3.3166 mL | |
| 20 mM | 0.0995 mL | 0.4975 mL | 0.9950 mL | 2.4874 mL | |
| 25 mM | 0.0796 mL | 0.3980 mL | 0.7960 mL | 1.9899 mL | |
| 30 mM | 0.0663 mL | 0.3317 mL | 0.6633 mL | 1.6583 mL | |
| 40 mM | 0.0497 mL | 0.2487 mL | 0.4975 mL | 1.2437 mL | |
| 50 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9950 mL | |
| 60 mM | 0.0332 mL | 0.1658 mL | 0.3317 mL | 0.8291 mL | |
| 80 mM | 0.0249 mL | 0.1244 mL | 0.2487 mL | 0.6219 mL | |
| 100 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4975 mL |
ZM223 Related Classifications
HY-101790 Related Classifications
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