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Cat. No.: HY-101790

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ZM223

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

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 2031177-48-5
Formule: C₂₃H₁₇F₃N₄O₂S₂
Masse moléculaire:502.53

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

ZM223 Chemical Structure

CAS No.: 2031177-48-5

Stock

Quantité

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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
A549	IC₅₀	41.23 μM Compound: ZM223	Antiproliferative activity against human A549 cells by CCK8 assay Antiproliferative activity against human A549 cells by CCK8 assay	[PMID: 38320715]
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]
KYSE-30	IC₅₀	17.38 μM Compound: ZM223	Antiproliferative activity against human KYSE-30 cells by CCK8 assay Antiproliferative activity against human KYSE-30 cells by CCK8 assay	[PMID: 38320715]
MCF7	IC₅₀	>100 μM Compound: ZM223	Antiproliferative activity against human MCF7 cells by CCK8 assay Antiproliferative activity against human MCF7 cells by CCK8 assay	[PMID: 38320715]
MGC-803	IC₅₀	4.91 μM Compound: ZM223	Antiproliferative activity against human MGC-803 cells by CCK8 assay Antiproliferative activity against human MGC-803 cells by CCK8 assay	[PMID: 38320715]
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.

Chemical Information

CAS No. 2031177-48-5
Masse moléculaire 502.53
Formule C₂₃H₁₇F₃N₄O₂S₂
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références

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ZM223

Activité biologique

Description

IC50 & Target

Cellular Effect

In Vitro

Chemical Information

Solvant et solubilité

In Vitro:

In Vivo:

In Vivo Dissolution Calculator

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ZM223 Related Classifications

HY-101790 Related Classifications

Bioz

Keywords

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