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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Eukaryotic Initiation Factor (eIF)-HR-19011
HR-19011

Chemical Structure : HR-19011

CAS No.: 2851820-52-3

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HR-19011 (HR19011)

货号: PC-24545Not For Human Use, Lab Use Only.

HR-19011 is a specific small molecule eIF2α phosphorylation inducer, increases the expression level of eIF2α downstream proteins, ATF and CHOP, shows antiproliferation in K562 cells with IC50 of 4.0 uM.

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5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HR-19011 is a specific small molecule eIF2α phosphorylation inducer, increases the expression level of eIF2α downstream proteins, ATF and CHOP, shows antiproliferation in K562 cells with IC50 of 4.0 uM.
HR-19011 exerts anticancer effects primarily through the activation of heme-regulated inhibitor (HRI), leading to the phosphorylation of eukaryotic translation initiation factor 2 (eIF2)α.
HR-19011 exhibits remarkably high selectivity index over PBMC cells.
HR-19011 increases the expression level of eIF2α downstream proteins, ATF and CHOP.
HR-19011 suppresses the mTORC1 pathway, a critical regulator of cell growth and metabolism, through the downregulation of components such as phosphorylated (p)-S6K and p-4EBP1, mediated by ATF4 and CHOP.
HR-19011 effectively inhibits tumor growth in a K562 xenograft model, without significant toxicity.

物理化学性质&存储条件

分子量 523.44
分子式 C25H19F6N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-((3,4-dioxo-2-(((1r,4r)-4-(4-(trifluoromethyl)phenoxy)cyclohexyl)amino)cyclobut-1-en-1-yl)amino)-5-(trifluoromethyl)benzonitrile

参考文献

1. Jinsook Kwak, et al. Eur J Med Chem. 2022 May 29;239:114501.

2. Kim MJ, et al. Mol Cancer Ther. 2025 Apr 28. doi: 10.1158/1535-7163.MCT-24-0998.

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