4EGI-1

製品コードS7369 バッチS736903

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H12Cl2N4O4S
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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro

4EGI-1 disrupts the eIF4F complex and inhibits Cap-dependent translation in vitro. This compound has proapoptotic activity in Jurkat cells, and potently inhibits cell growth with IC50 of approximately 6 μM in A549 lung cancer cells. [1] It 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, this chemical restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. [3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Jurkat cells and A549 lung cancer cells.
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 of this compound 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 treatment with this compound is visualized by staining of cells with Hoechst dye and fluorescence microscopy. For the A549 lung cancer cells, cell growth in the presence of this chemical is determined using the SRB staining method.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17254965/
  • https://pubmed.ncbi.nlm.nih.gov/20360945/
  • https://pubmed.ncbi.nlm.nih.gov/23633452/
  • https://pubmed.ncbi.nlm.nih.gov/28797827

カスタマーフィードバック

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.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

mTORC1 regulates cell survival under glucose starvation through 4EBP1/2-mediated translational reprogramming of fatty acid metabolism [ Nat Commun, 2024, 15(1):4083] PubMed: 38744825
mTORC1 regulates cell survival under glucose starvation through 4EBP1/2-mediated translational reprogramming of fatty acid metabolism [ Nat Commun, 2024, 15(1):4083] PubMed: 38744825
Ribosome Quality Control mitigates the cytotoxicity of ribosome collisions induced by 5-Fluorouracil [ Nucleic Acids Res, 2024, gkae849] PubMed: 39351862
Mechanistic differences in eukaryotic initiation factor requirements for eIF4GI-driven cap-independent translation of structured mRNAs [ J Biol Chem, 2024, 300(11):107866] PubMed: 39384039
A drug discovery pipeline for MAPK/ERK pathway inhibitors in C. elegans [ Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221] PubMed: 39212544
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
LRG1 is a novel HER3 ligand to promote growth in colorectal cancer [ bioRxiv, 2023, PPR618443 ] PubMed: none
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

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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