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| 1mg |
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| 5mg |
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| Targets |
eIF2
EIF2α activator 1 targets the eukaryotic initiation factor 2α (eIF2α), a key regulator of protein synthesis. Phosphorylation of eIF2α at serine 51 inhibits global protein synthesis while selectively promoting the translation of stress-responsive mRNAs such as ATF4, which in turn induces the expression of downstream proteins ATF and CHOP. By activating eIF2α phosphorylation, the compound induces the integrated stress response (ISR), which can lead to cell cycle arrest and apoptosis in cancer cells. |
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| ln Vitro |
In vitro, EIF2α activator 1 increases the expression levels of eIF2α downstream proteins ATF and CHOP. The compound exhibits anti-proliferative activity against K562 cells with an IC₅₀ of 4.00 μM and against PBMC cells with an IC₅₀ of 19.3 μM. Its ability to activate eIF2α phosphorylation and induce the integrated stress response makes it a valuable tool for studying the role of eIF2α in cancer and other diseases.
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| ln Vivo |
In vivo activity data for EIF2α activator 1 are limited. As an activator of eIF2α phosphorylation with anti-proliferative activity, the compound may have potential for in vivo studies in animal models of cancer. Typical in vivo studies involve administration to tumor-bearing mouse models, with assessment of tumor growth inhibition and eIF2α phosphorylation markers.
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| Enzyme Assay |
For non-cellular in vitro assays, EIF2α activator 1 is evaluated for its ability to activate eIF2α phosphorylation. The compound is incubated with purified eIF2α and its upstream kinases (such as PERK, PKR, GCN2, or HRI), and the phosphorylation of eIF2α is measured using phospho-specific antibodies or radioactive labeling.
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| Cell Assay |
For in vitro cellular assays, EIF2α activator 1 is tested in cancer cell lines such as K562 cells. Cells are treated with serial dilutions of the compound, and eIF2α phosphorylation is measured by Western blot using phospho-eIF2α (Ser51) antibodies. Expression of downstream proteins ATF and CHOP is assessed. Cell viability and proliferation are measured using standard assays.
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| Animal Protocol |
For in vivo animal studies, EIF2α activator 1 would typically be evaluated in xenograft mouse models of cancer. Mice bearing established tumors are treated with the compound via oral or intraperitoneal administration. Tumor volumes are measured regularly, and tumor growth inhibition is calculated. eIF2α phosphorylation and downstream protein expression are assessed in tumor tissues at study endpoint. Body weight and general health are monitored to evaluate tolerability.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for EIF2α activator 1 are limited. As a small-molecule activator with a molecular weight of 523.43, it is expected to have moderate oral bioavailability and tissue distribution. The compound is soluble in DMSO and can be formulated for in vivo administration. Further pharmacokinetic studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for EIF2α activator 1 are limited. As an activator of eIF2α phosphorylation that induces the integrated stress response, the compound may have on-target effects on normal cellular protein synthesis and stress responses. Comprehensive toxicology studies including acute and repeat-dose toxicity, genotoxicity, and organ-specific toxicity assessments would be required for therapeutic development. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
EIF2α activator 1 (Compound 40) is an activator of eIF2α phosphorylation that increases the expression of downstream proteins ATF and CHOP. The compound exhibits anti-proliferative activity against K562 cells with an IC₅₀ of 4.00 μM and against PBMC cells with an IC₅₀ of 19.3 μM. It has a molecular formula of C₂₅H₁₉F₆N₃O₃ and a molecular weight of 523.43. EIF2α activator 1 is a valuable tool for studying the integrated stress response in cancer research.
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| Molecular Formula |
C25H19F6N3O3
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|---|---|
| Molecular Weight |
523.43
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| Exact Mass |
523.133
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| CAS # |
2851820-52-3
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| PubChem CID |
164517084
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| Appearance |
White to yellow solid powder
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| Density |
1.47±0.1 g/cm3(Predicted)
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| Boiling Point |
561.4±60.0 °C(Predicted)
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| LogP |
6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
953
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(CCC1NC2=C(C(=O)C2=O)NC3=CC(=CC(=C3)C(F)(F)F)C#N)OC4=CC=C(C=C4)C(F)(F)F
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| InChi Key |
PYDUAMACJGQTQN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19F6N3O3/c26-24(27,28)14-1-5-18(6-2-14)37-19-7-3-16(4-8-19)33-20-21(23(36)22(20)35)34-17-10-13(12-32)9-15(11-17)25(29,30)31/h1-2,5-6,9-11,16,19,33-34H,3-4,7-8H2
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| Chemical Name |
3-[[3,4-dioxo-2-[[4-[4-(trifluoromethyl)phenoxy]cyclohexyl]amino]cyclobuten-1-yl]amino]-5-(trifluoromethyl)benzonitrile
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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: 25 mg/mL (47.76 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9105 mL | 9.5524 mL | 19.1048 mL | |
| 5 mM | 0.3821 mL | 1.9105 mL | 3.8210 mL | |
| 10 mM | 0.1910 mL | 0.9552 mL | 1.9105 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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