GCN2-IN-1
Based on 27 publication(s) in Google Scholar
GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 1448693-69-3
- Formula: C19H18N10O
- Molecular Weight:402.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GCN2-IN-1
More- Nat Cell Biol. 2025 Nov;27(11):1889-1901. [Abstract]
- Mol Cell. 2023 Dec 7;83(23):4290-4303.e9. [Abstract]
- Nat Commun. 2023 Oct 25;14(1):6777. [Abstract]
- Nat Commun. 2023 Sep 8;14(1):5535. [Abstract]
- Cell Death Differ. 2023 Jul;30(7):1666-1678. [Abstract]
- Neuron. 2019 Nov 20;104(4):724-735.e6. [Abstract]
- Nucleic Acids Res. 2024 May 22;52(9):5356-5375. [Abstract]
- Cell Discov. 2021 Oct 26;7(1):98. [Abstract]
- Cell Death Dis. 2022 Nov 18;13(11):969. [Abstract]
- EMBO Rep. 2023 Aug 3;24(8):e56100. [Abstract]
- JCI Insight. 2024 Sep 24;9(20):e177926. [Abstract]
- Front Microbiol. 2021 Apr 12:12:624540. [Abstract]
- FASEB J. 2022 Mar;36(3):e22201. [Abstract]
- J Biol Chem. 2023 Apr;299(4):104595 [Abstract]
- J Cell Sci. 2022 Jul 15;135(14):jcs259629. [Abstract]
- Am J Physiol Gastrointest Liver Physiol. 2025 Apr 17. [Abstract]
- Dis Model Mech. 2024 Aug 14:dmm.050748. [Abstract]
- Res Vet Sci. 2025 May:187:105603. [Abstract]
- Biol Open. 2022 Feb 15;11(2):bio058728. [Abstract]
- bioRxiv. 2026 May 29:2026.05.26.727520. [Abstract]
- bioRxiv. 2026 Apr 21.
- bioRxiv. 2025 March 19.
- bioRxiv. 2024 August 16.
- University of Maryland. 2024.
- Research Square Preprint. 2024 Feb 14.
- Research Square Preprint. 2021 Oct.
- bioRxiv. 2020 Apr.
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Cell Imaging/Staining
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Biological Activity
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eIF2 |
Chemical Information
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CAS No. 1448693-69-3
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Appearance Solid
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Molecular Weight 402.41
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Formula C19H18N10O
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Color Light yellow to yellow
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SMILES
C1(NC2=CN(C3CCOCC3)N=C2)=NC=C(N=NN4C5=CC6=C(C=C5)C=NN6)C4=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (27)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
Leucine inhibits degradation of outer mitochondrial membrane proteins to adapt mitochondrial respiration. [Abstract]2025 Nov;27(11):1889-1901. PMID: 41174002
GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2025 Nov;27(11):1889-1901. [Abstract]
Ubiquitylation of whole-cell proteins and OMM proteins of cells cultured in medium supplemented with 0 mM or 1 mM Leu and/or 0 µM or 10 µM GCN2-IN-1 for 3 h. For each sample, 10 µg proteins were loaded. Ubiquitylation levels were normalized to the total OMM protein amount.
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Mol Cell
RNF14-dependent atypical ubiquitylation promotes translation-coupled resolution of RNA-protein crosslinks. [Abstract]2023 Dec 7;83(23):4290-4303.e9. PMID: 37951216 -
Nat Commun
Mutant p53 sustains serine-glycine synthesis and essential amino acids intake promoting breast cancer growth. [Abstract]2023 Oct 25;14(1):6777. PMID: 37880212
GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 25;14(1):6777. [Abstract]
MDA-MB 231 cells were cultured for 72 hours in complete medium (CM) and medium containing 25% amino acids (low amino acid). Then, they were treated with (+) or (-) 1 μM GCN2-IN-1 for 72 hours, respectively, and Western blot analysis was performed to detect the expression of the proteins shown.
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Nat Commun
2023 Sep 8;14(1):5535. PMID: 37684277
GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 8;14(1):5535. [Abstract]
After treating HeLa cells with the GCN2 inhibitor GCN2-IN-1 (A92) at progressively increasing concentrations for 5 hours, the specified proteins in the lysate were analyzed by immunoblotting.
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Cell Death Differ
Actionable cancer vulnerability due to translational arrest, p53 aggregation and ribosome biogenesis stress evoked by the disulfiram metabolite CuET. [Abstract]2023 Jul;30(7):1666-1678. PMID: 37142656
GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jul;30(7):1666-1678. [Abstract]
Immunoblotting of phosphorylated eIF2a (ser51) following treatment of A549 with CuET (2 h) +/–PERK inhibitor combined with siRNA against HRI or GCN2-IN-1 (10 μM; 30 min). Numbers below the blot indicate the signal ratio p-eIF2a/β-actin.
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Neuron
The eIF2α Kinase GCN2 Modulates Period and Rhythmicity of the Circadian Clock by Translational Control of Atf4. [Abstract]2019 Nov 20;104(4):724-735.e6. PMID: 31522764 -
Nucleic Acids Res
2024 May 22;52(9):5356-5375. PMID: 38366783
GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2024 May 22;52(9):5356-5375. [Abstract]
U2OS cells were treated with a PERK inhibitor (GSK II, 40 μM), or with GCN2-IN-1 (4 μM), for 3 h prior to transfection. mRNA (1 μg) encoding GFP (green) was transfected, and cells were fixed 1.5 h post-transfection. Cells were stained using anti-G3BP1 (magenta).
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Cell Discov
Selective and competitive functions of the AAR and UPR pathways in stress-induced angiogenesis. [Abstract]2021 Oct 26;7(1):98. PMID: 34697290 -
Cell Death Dis
An mTORC1 to HRI signaling axis promotes cytotoxicity of proteasome inhibitors in multiple myeloma. [Abstract]2022 Nov 18;13(11):969. PMID: 36400754 -
EMBO Rep
2023 Aug 3;24(8):e56100. PMID: 37291955 -
JCI Insight
GCN2 kinase activation mediates pulmonary vascular remodeling and pulmonary arterial hypertension. [Abstract]2024 Sep 24;9(20):e177926. PMID: 39316438 -
Front Microbiol
Duck Hepatitis A Virus Type 1 Induces eIF2α Phosphorylation-Dependent Cellular Translation Shutoff via PERK/GCN2. [Abstract]2021 Apr 12:12:624540. PMID: 33912143 -
FASEB J
Amino acid restriction induces a long non-coding RNA UBA6-AS1 to regulate GCN2-mediated integrated stress response in breast cancer. [Abstract]2022 Mar;36(3):e22201. PMID: 35137449 -
J Biol Chem
2023 Apr;299(4):104595 PMID: 36898579 -
J Cell Sci
Glucocorticoids enhance chemotherapy-driven stress granule assembly and impair granule dynamics, leading to cell death. [Abstract]2022 Jul 15;135(14):jcs259629. PMID: 35713120 -
Am J Physiol Gastrointest Liver Physiol
Saturated phosphatidic acids induce mTORC1-driven integrated stress response contributing to glucolipotoxicity in hepatocytes. [Abstract]2025 Apr 17. PMID: 40241617 -
Dis Model Mech
2024 Aug 14:dmm.050748. PMID: 39139065 -
Res Vet Sci
Sodium ferrous citrate in 5-Aminolevulinic acid supplements suppresses the effector function of feline lymphocytes by reducing the mitochondrial membrane potential. [Abstract]2025 May:187:105603. PMID: 40048774 -
Biol Open
2022 Feb 15;11(2):bio058728. PMID: 34994382 -
bioRxiv
2026 May 29:2026.05.26.727520. PMID: 42244578 -
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Solvent & Solubility
DMSO : 50 mg/mL (124.25 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: ≥ 2.5 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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Data Sheet (272 KB)
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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)
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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 | 2.4850 mL | 12.4251 mL | 24.8503 mL | 62.1257 mL |
| 5 mM | 0.4970 mL | 2.4850 mL | 4.9701 mL | 12.4251 mL | |
| 10 mM | 0.2485 mL | 1.2425 mL | 2.4850 mL | 6.2126 mL | |
| 15 mM | 0.1657 mL | 0.8283 mL | 1.6567 mL | 4.1417 mL | |
| 20 mM | 0.1243 mL | 0.6213 mL | 1.2425 mL | 3.1063 mL | |
| 25 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4850 mL | |
| 30 mM | 0.0828 mL | 0.4142 mL | 0.8283 mL | 2.0709 mL | |
| 40 mM | 0.0621 mL | 0.3106 mL | 0.6213 mL | 1.5531 mL | |
| 50 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2425 mL | |
| 60 mM | 0.0414 mL | 0.2071 mL | 0.4142 mL | 1.0354 mL | |
| 80 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7766 mL | |
| 100 mM | 0.0249 mL | 0.1243 mL | 0.2485 mL | 0.6213 mL |