2. Metabolic Enzyme/Protease
  3. NEDD8-activating Enzyme
  4. ZM223

ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (ZM223 hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

ZM223 Chemical Structure

ZM223 Chemical Structure

CAS No. : 2031177-48-5

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ZM223 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active[1].

IC50 & Target

NEDD8 activating enzyme (NAE)[1]
In Vitro

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.

ZM223 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT116 colon cancer cells and U-2OS osteosarcoma cells
Concentration: 0.1 μM, 1 μM
Incubation Time: 4 hours
Result: Inhibited both HCT-116 and U-2OS cancer cells.

Western Blot Analysis[1]

Cell Line: HCT116 colon cancer cells
Concentration: 0.1 μM, 1 μM
Incubation Time: 4 hours
Result: Caused a decrease in the level of NEDD8 and an increase in the downstream UBC12 protein.
Molecular Weight

502.53

Formula

C23H17F3N4O2S2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9899 mL 9.9497 mL 19.8993 mL
5 mM 0.3980 mL 1.9899 mL 3.9799 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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ZM223 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZM2232031177-48-5ZM 223ZM-223NEDD8-activating EnzymeNAEInhibitorinhibitorinhibit

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