GCN2-IN-1 (A-92) (Synonyms: A-92, GCN2 Inhibitor 1, General Control Nonderepressible 2 Kinase Inhibitor 1) |
| Catalog No.GC32771 |
GCN2-IN-1 (A-92) (A-92) 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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448693-69-3
Sample solution is provided at 25 µL, 10mM.
GCN2-IN-1 is an inhibitor of general control nonderepressible 2 kinase (GCN2; IC50 = ~0.2 μM for autophosphorylation), a serine/threonine protein kinase involved in the integrated stress response.1 It also inhibits integrase phosphorylation (IC50 = ~0.2 μM for the HIV-1 enzyme). GCN2-IN-1 inhibits ELAV-like protein 1, also known as human antigen R (HuR), protein dimerization (IC50 = 4.5 μM).2 GCN2-IN-1 also decreases the viability of U251, XD456, U87, and LN-229 glioma cells (IC50s = 4.7, 2.8, 3.2, and 2.7 μM, respectively).
References:
1.Torres, C., Garling, A., Taouji, S., et al.Targeting the integrated stress response kinase GCN2 to modulate retroviral integrationMolecules26(17)5423(2021)
2.Filippova, N., Yang, X., Ananthan, S., et al.Targeting the HuR oncogenic role with a new class of cytoplasmic dimerization inhibitorsCancer Res.81(8)2220-2233(2021)
| Cas No. | 1448693-69-3 | SDF | |
| Synonyms | A-92, GCN2 Inhibitor 1, General Control Nonderepressible 2 Kinase Inhibitor 1 | ||
| Canonical SMILES | C1(NC2=CN(C3CCOCC3)N=C2)=NC=C(N=NN4C5=CC6=C(C=C5)C=NN6)C4=N1 | ||
| Formula | C19H18N10O | M.Wt | 402.41 |
| Solubility | DMSO : 60 mg/mL (149.10 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.485 mL | 12.4251 mL | 24.8503 mL |
| 5 mM | 497 μL | 2.485 mL | 4.9701 mL |
| 10 mM | 248.5 μL | 1.2425 mL | 2.485 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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