ZM223

Cat. No.: HY-101790: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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

CAS No. : 2031177-48-5

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Other Forms of ZM223:

ZM223 hydrochloride Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

NEDD8 activating enzyme (NAE)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.1 μM Compound: 7g; ZM223	Antitumor activity against human HCT116 cells after 72 hrs by MTT assay Antitumor activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28388520]
U2OS	IC₅₀	1.22 μM Compound: 7g; ZM223	Antitumor activity against human U2OS cells after 72 hrs by MTT assay Antitumor activity against human U2OS cells after 72 hrs by MTT assay	[PMID: 28388520]

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.

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.

2031177-48-5

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
10 mM	0.1990 mL	0.9950 mL	1.9899 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

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

Handling Instructions (2659 KB)

References

[1]. Ma H, et al. Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening. Eur J Med Chem. 2017 Jun 16;133:174-183. [Content Brief]

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

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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