GCN2-IN-6
Based on 3 publication(s) in Google Scholar
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells). GCN2-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity: 98.89%
- CAS No.: 2183470-09-7
- Formula: C19H12Cl2F2N4O3S
- Molecular Weight:485.29
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Endoplasmic Reticulum Stress Compound Library
HY-L054
-
Orally Active Compound Library
HY-L061
-
Anti-Blood Cancer Compound Library
HY-L079
-
Targeted Diversity Library
HY-L099
-
Anti-Hematopathy Compound Library
HY-L171
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Alkyne Compound Library
HY-L258
Publications Citing Use of MedChemExpress (MCE) GCN2-IN-6
More
Biological Activity
|
eIF2 |
To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF. GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mice bearing CCRF-CEM cells xenografts[1]
-
Dosage:0.3 mg/kg, 1 mg/kg, and 3 mg/kg
-
Administration:Oral administration; for 8 hours
-
Result:Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.
Chemical Information
-
CAS No. 2183470-09-7
-
Appearance Solid
-
Molecular Weight 485.29
-
Formula C19H12Cl2F2N4O3S
-
Color Light yellow to yellow
-
SMILES
O=S(C1=CC(Cl)=CC(CO)=C1Cl)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Mol Cell
2022 Mar 3;82(5):920-932.e7. PMID: 35245456 -
Blood Cancer Discov
Translational Activation of ATF4 through Mitochondrial Anaplerotic Metabolic Pathways Is Required for DLBCL Growth and Survival. [Abstract]2022 Jan;3(1):50-65. PMID: 35019856 -
Solvent & Solubility
DMSO : 250 mg/mL (515.16 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (4.29 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.
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.
Purity & Documentation
-
Data Sheet (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0606 mL | 10.3031 mL | 20.6062 mL | 51.5156 mL |
| 5 mM | 0.4121 mL | 2.0606 mL | 4.1212 mL | 10.3031 mL | |
| 10 mM | 0.2061 mL | 1.0303 mL | 2.0606 mL | 5.1516 mL | |
| 15 mM | 0.1374 mL | 0.6869 mL | 1.3737 mL | 3.4344 mL | |
| 20 mM | 0.1030 mL | 0.5152 mL | 1.0303 mL | 2.5758 mL | |
| 25 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0606 mL | |
| 30 mM | 0.0687 mL | 0.3434 mL | 0.6869 mL | 1.7172 mL | |
| 40 mM | 0.0515 mL | 0.2576 mL | 0.5152 mL | 1.2879 mL | |
| 50 mM | 0.0412 mL | 0.2061 mL | 0.4121 mL | 1.0303 mL | |
| 60 mM | 0.0343 mL | 0.1717 mL | 0.3434 mL | 0.8586 mL | |
| 80 mM | 0.0258 mL | 0.1288 mL | 0.2576 mL | 0.6439 mL | |
| 100 mM | 0.0206 mL | 0.1030 mL | 0.2061 mL | 0.5152 mL |
Powered by Bioz