受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H12Cl2N4O4S |
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分子量 | 451.28 | CAS No. | 315706-13-9 | |
Solubility (25°C)* | 体外 | DMSO | 90 mg/mL (199.43 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis. |
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in vitro | 4EGI-1 disrupts the eIF4F complex and inhibits Cap-dependent translation in vitro. 4EGI-1 has proapoptotic activity in Jurkat cells, and potently inhibits cell growth with IC50 of approximately 6 μM in A549 lung cancer cells. [1] 4EGI-1 augments TRAIL-induced apoptosis through induction of DR5 and down-regulation of c-FLIP, independent of inhibition of cap-dependent protein translation in human lung cancer cells. [2] In addition, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. [3] |
細胞アッセイ | 細胞株 | Jurkat cells and A549 lung cancer cells. |
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濃度 | ~60 μM | |
反応時間 | 24 hours | |
実験の流れ | Cell viability is measured by treatment of Jurkat cells with compound for 24 h and by determination of intracellular ATP using the CellTiterGlo assay. For measurement of apoptotic DNA fragmentation, cells are treated for 24 h with 60 μM EGI-1 or 6.65 μM camptothecin in the presence or absence of 100 mM zVAD-FMK, a broad-spectrum caspase inhibitor. After fixation and staining with PI, cellular DNA content is determined by FACS analysis in a FACS Calibur machine. Nuclear morphology after 24 h EG1-1 treatment is visualized by staining of cells with Hoechst dye and fluorescence microscopy. For the A549 lung cancer cells, cell growth in the presence of 4EGI-1 is determined using the SRB staining method. |
Data from [Data independently produced by , , Mol Cancer Ther, 2017, 16(9):1806-1818]
Data from [Data independently produced by , , Int J Oncol, 2015, 47(6):2217-25.]
DEAD-Box Helicase 17 Promotes Amyloidogenesis by Regulating BACE1 Translation [ Brain Sci, 2023, 13(5)745] | PubMed: 37239217 |
DEAD-Box Helicase 17 Promotes Amyloidogenesis by Regulating BACE1 Translation [ Brain Sci, 2023, 13(5)745] | PubMed: 37239217 |
Surgical Reconstruction of Stage 3 and 4 Pressure Injuries: A Literature Review and Proposed Algorithm from an Interprofessional Working Group [ Adv Skin Wound Care, 2023, 36(5):249-258] | PubMed: 37079788 |
Ribosome Quality Control Mechanism Mitigates the Cytotoxic Impacts of Ribosome Collisions Induced by 5-Fluorouracil [ bioRxiv, 2023, 10.1101/2023.12.26.573247] | PubMed: none |
Dephosphorylation of 4EBP1/2 Induces Prenatal Neural Stem Cell Quiescence [ bioRxiv, 2023, 2023.02.14.528513] | PubMed: 36824760 |
Retinoic acid and RARγ maintain satellite cell quiescence through regulation of translation initiation [ Cell Death Dis, 2022, 13-9:838] | PubMed: 36175396 |
Role of EIF4G1 network in non-small cell lung cancers (NSCLC) cell survival and disease progression [ J Cell Mol Med, 2021, 10.1111/jcmm.16307] | PubMed: 33539648 |
TUFM is involved in Alzheimer's disease-like pathologies that are associated with ROS [ FASEB J, 2021, 35(5):e21445] | PubMed: 33774866 |
Berberine Represses β-Catenin Translation Involving 4E-BPs in Hepatocellular Carcinoma Cells [ Mol Pharmacol, 2021, 99(1):1-16] | PubMed: 33130557 |
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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