NAE-IN-M22
Based on 1 Customer Validation
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.94%
- CAS No.: 864420-54-2
- Formule: C20H24Cl2N2
- Masse moléculaire:363.32
-
Stockage: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]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
NEDD8 activating enzyme (NAE)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
5.55 μM
Compound: 7; M22
|
Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
|
[PMID: 29843100] |
| AGS | IC50 |
9.92 μM
Compound: 7; M22
|
Antiproliferative activity against human AGS cells after 48 hrs by CCK8 assay
Antiproliferative activity against human AGS cells after 48 hrs by CCK8 assay
|
[PMID: 29843100] |
| BXPC-3 | IC50 |
12.4 μM
Compound: 7; M22
|
Antiproliferative activity against human BxPC3 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human BxPC3 cells after 48 hrs by CCK8 assay
|
[PMID: 29843100] |
| HCT-116 | IC50 |
10.57 μM
Compound: 7; M22
|
Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay
|
[PMID: 29843100] |
| K562 | IC50 |
5.51 μM
Compound: 7; M22
|
Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
|
[PMID: 29843100] |
| SK-OV-3 | IC50 |
9.26 μM
Compound: 7; M22
|
Antiproliferative activity against human SKOV3 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human SKOV3 cells after 48 hrs by CCK8 assay
|
[PMID: 29843100] |
M22 (0.37-90 μM; 24 h) blocks neddylation pathway selectively and suppresses degradation of CRL substrates in A549 cells[1].
M22 (0.1-100 μM; 48 h) inhibits A549 cell proliferation completely at 30 µM (GI50=5.5 µM, GI90=19.3 µM)[1].
M22 (15-30 μM; 36 h) promotes apoptosis in A549 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549 cells
-
Concentration:0.37, 1.11, 3.33, 10, 30, 90 μM
-
Incubation Time:24 hours
-
Result:Inhibited formations of Uba3-NEDD8 and Ubc12-NEDD8.
Resulted in a corresponding decrease in the abundance of Cullins-NEDD8.
Decreased the degradations of p27 and CDT1.
Prevented p53 from degradation.
Chemical Information
-
CAS No. 864420-54-2
-
Appearance Solid
-
Masse moléculaire 363.32
-
Formule C20H24Cl2N2
-
Color White to off-white
-
SMILES
ClC1=CC=C(CCNC2CCN(CC3=CC=CC=C3)CC2)C(Cl)=C1
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 250 mg/mL (688.10 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: ≥ 2.08 mg/mL (5.72 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.72 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 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:
-
-
-
-
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
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.
Pureté et documentation
-
Fiche technique (271 KB)
-
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)
-
Instruction de manipulation (2659 KB)
Références
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 | 2.7524 mL | 13.7620 mL | 27.5239 mL | 68.8099 mL |
| 5 mM | 0.5505 mL | 2.7524 mL | 5.5048 mL | 13.7620 mL | |
| 10 mM | 0.2752 mL | 1.3762 mL | 2.7524 mL | 6.8810 mL | |
| 15 mM | 0.1835 mL | 0.9175 mL | 1.8349 mL | 4.5873 mL | |
| 20 mM | 0.1376 mL | 0.6881 mL | 1.3762 mL | 3.4405 mL | |
| 25 mM | 0.1101 mL | 0.5505 mL | 1.1010 mL | 2.7524 mL | |
| 30 mM | 0.0917 mL | 0.4587 mL | 0.9175 mL | 2.2937 mL | |
| 40 mM | 0.0688 mL | 0.3440 mL | 0.6881 mL | 1.7202 mL | |
| 50 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL | 1.3762 mL | |
| 60 mM | 0.0459 mL | 0.2294 mL | 0.4587 mL | 1.1468 mL | |
| 80 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8601 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6881 mL |
NAE-IN-M22 Related Classifications
HY-115537 Related Classifications
Powered by Bioz