ATF4-IN-2
Based on 1 Customer Validation
ATF4-IN-2 is an ATF4 inhibitor with an IC50 of 47.71 nM. ATF4-IN-2 activates eIF2B, binds to the ISRIB (HY-12495A) binding pocket, restores protein translation, and inhibits ATF4 expression. ATF4-IN-2 inhibits ATF4 protein expression in Thapsigargin (HY-13433)-stimulated cells. ATF4-IN-2 can be used for research on neurodegenerative diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.24%
- CAS. Nr.: 2991057-60-2
- Formel: C24H21BrClN5O4
- Molecular Weight:558.81
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
ATF4 47.71 nM (IC50) |
eIF2B 37.70 nM (EC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
21.29 μM
|
Antiproliferative activity against thapsigargin-stimulated HEK-293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against thapsigargin-stimulated HEK-293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
|
38426720 |
In Vitro
ATF4-IN-2 (compound 29) (1-1000 nM; 3 h) exhibited a satisfactory 88.7% inhibition rate of ATF4 in Thapsigargin-stimulated HEK-293T cells[1].
ATF4-IN-2 (3 h) inhibits ATF4 expression in Thapsigargin-stimulated HEK-293T cells in a dose-dependent manner with an IC50 of 47.71 nM[1].
ATF4-IN-2 (200 nM; 3 h) effectively inhibits ATF4 mRNA transcription and restores it to normal levels in Thapsigargin-stimulated HeLa cells[1].
ATF4-IN-2 (6 h) activates eIF2B with an EC50 of 37.70 nM in HEK-293T cells carrying an ATF4 Nano-Luciferase reporter[1].
ATF4-IN-2 (48 h) exhibits low cytotoxicity against HEK-293T cells, with an IC50 of 21.29 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK-293T
-
Concentration:1 nM; 10 nM; 100 nM; 500 nM; 1000 nM
-
Incubation Time:3 h
-
Result:Exhibited an ATF4 inhibition rate of 88.7%.
-
Cell Line:HeLa
-
Concentration:200 nM
-
Incubation Time:3 h
-
Result:Effectively inhibited the transcription of ATF4 mRNA.
Chemical Information
-
CAS. Nr. 2991057-60-2
-
Appearance Solid
-
Molecular Weight 558.81
-
Formel C24H21BrClN5O4
-
Color White to off-white
-
SMILES
O=C(C1=NN=C(C2=CC=C(Br)C=C2)O1)NCC3CCN(NC(C4=CC5=CC(Cl)=CC=C5O4)=O)CC3
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (178.95 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
-
Data Sheet (279 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
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 | 1.7895 mL | 8.9476 mL | 17.8952 mL | 44.7379 mL |
| 5 mM | 0.3579 mL | 1.7895 mL | 3.5790 mL | 8.9476 mL | |
| 10 mM | 0.1790 mL | 0.8948 mL | 1.7895 mL | 4.4738 mL | |
| 15 mM | 0.1193 mL | 0.5965 mL | 1.1930 mL | 2.9825 mL | |
| 20 mM | 0.0895 mL | 0.4474 mL | 0.8948 mL | 2.2369 mL | |
| 25 mM | 0.0716 mL | 0.3579 mL | 0.7158 mL | 1.7895 mL | |
| 30 mM | 0.0597 mL | 0.2983 mL | 0.5965 mL | 1.4913 mL | |
| 40 mM | 0.0447 mL | 0.2237 mL | 0.4474 mL | 1.1184 mL | |
| 50 mM | 0.0358 mL | 0.1790 mL | 0.3579 mL | 0.8948 mL | |
| 60 mM | 0.0298 mL | 0.1491 mL | 0.2983 mL | 0.7456 mL | |
| 80 mM | 0.0224 mL | 0.1118 mL | 0.2237 mL | 0.5592 mL | |
| 100 mM | 0.0179 mL | 0.0895 mL | 0.1790 mL | 0.4474 mL |