| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GCN2 modulator-1 targets general control nonderepressible 2 (GCN2), a serine/threonine protein kinase that is activated in response to amino acid deprivation and other stress signals. GCN2 phosphorylates eukaryotic initiation factor 2α (eIF2α), leading to attenuation of global protein synthesis and activation of the integrated stress response. By inhibiting GCN2 with an IC50 of less than 0.05 μM, the compound modulates this stress response pathway, which is important in anti-tumor research.
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| ln Vitro |
In vitro studies demonstrate that GCN2 modulator-1 is a potent inhibitor of GCN2 with an IC50 value of less than 0.05 μM. This high potency indicates strong inhibitory activity against the kinase. The compound plays an important role in anti-tumor research. Detailed in vitro activity data, including cellular phosphorylation assays and effects on cancer cell lines, are not extensively documented in the available literature. The compound is also known as HC-7366.
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| ln Vivo |
In vivo activity of GCN2 modulator-1 is inferred from its role in anti-tumor research. As an inhibitor of GCN2, it may modulate the integrated stress response and affect tumor growth and survival. Detailed in vivo efficacy data from animal models, including tumor growth inhibition studies, are not extensively documented in the available literature. The compound is intended for research use only.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for GCN2 modulator-1 involves measuring its inhibitory activity against GCN2 kinase. The assay typically uses purified recombinant GCN2 enzyme incubated with the compound at varying concentrations, along with ATP and a substrate such as eIF2α. Kinase activity is measured by quantifying phosphorylation levels using methods such as radiometric assays, fluorescence polarization, or ELISA-based detection. IC50 values are determined by plotting percentage inhibition against compound concentration.
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| Cell Assay |
In vitro cell-based assays for GCN2 modulator-1 are conducted using cancer cell lines to evaluate its effects on the integrated stress response. Cells are treated with the compound at various concentrations, and GCN2 activity is assessed by measuring eIF2α phosphorylation by Western blot. Cell viability, proliferation, and apoptosis are evaluated using standard assays. The compound's ability to modulate stress responses and affect tumor cell survival is investigated.
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| Animal Protocol |
In vivo animal studies for GCN2 modulator-1 would typically be conducted using xenograft mouse models of cancer. Tumor-bearing mice would be administered the compound via appropriate routes, and tumor growth inhibition would be monitored. GCN2 activity and eIF2α phosphorylation in tumor tissues would be assessed by Western blot. Pharmacokinetic parameters would be determined from plasma samples. However, detailed protocols and efficacy data are not available from the search results.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GCN2 modulator-1 include its appearance as a white to off-white solid powder. Solubility includes DMSO at approximately 31.25 mg/mL (~61.41 mM). Storage recommendations include powder at -20°C for 3 years or 4°C for 2 years, and in solvent at -80°C for 6 months or -20°C for 1 month. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively documented.
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| Toxicity/Toxicokinetics |
Toxicity information for GCN2 modulator-1 is limited. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
GCN2 modulator-1 (compound 3, HC-7366) is a GCN2 inhibitor with an IC50 of less than 0.05 μM. It plays an important role in anti-tumor research. The compound has CAS number 2803470-63-3 and appears as a white to off-white solid powder. It is intended for research use only.
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| Exact Mass |
508.053
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| CAS # |
2803470-63-3
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| PubChem CID |
164593978
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
838
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC(=O)C1=C2C=NC(=CN2C=N1)C3=C(C=CC(=C3F)NS(=O)(=O)C4=C(N=CC(=C4)Cl)OC)F
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| InChi Key |
KIGXQRBUVDDSPP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15ClF2N6O4S/c1-24-19(30)18-14-7-25-13(8-29(14)9-27-18)16-11(22)3-4-12(17(16)23)28-34(31,32)15-5-10(21)6-26-20(15)33-2/h3-9,28H,1-2H3,(H,24,30)
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| Chemical Name |
6-[3-[(5-chloro-2-methoxy-3-pyridinyl)sulfonylamino]-2,6-difluorophenyl]-N-methylimidazo[1,5-a]pyrazine-1-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~31.25 mg/mL (~61.41 mM; with sonication (<60°C))
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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