吐根酚碱 TN1480

Product Introduction
Bioactivity


英文名: Cephaeline

描述: Cephaeline 对受保护的原代 CLL 细胞具有高度活性（相对 IC50 为 35nM），并通过抑制 HIF-1α± 和扰乱细胞内氧化还原稳态发挥作用。

体外活性: We compared the transcriptomes of primary CLL cells cocultured or not with protective bone marrow stromal cells (BMSCs) and found that oxidative phosphorylation, mitochondrial function, and hypoxic signaling undergo most significant dysregulation in non-protected CLL cells, with the changes peaking at 6-8 h, directly before induction of apoptosis. A subset of CLL patients displayed a gene expression signature resembling that of cocultured CLL cells and had significantly worse progression-free and overall survival. To identify drugs blocking BMSC-mediated support, we compared the relevant transcriptomic changes to the Connectivity Map database. Correlation was found with the transcriptomic signatures of the cardiac glycoside ouabain and of the ipecac alkaloids emetine and Cephaeline. These compounds were highly active against protected primary CLL cells (relative IC50's 287, 190, and 35 nM, respectively) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis. We tested emetine in a murine model of CLL and observed decreased CLL cells in peripheral blood, spleen, and bone marrow, recovery of hematological parameters and doubling of median survival (31.5 vs. 15 days, P = 0.0001).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 33.33 mg/mL (71.43 mM)


关键字: NSC 32944 | inhibit | Inhibitor | NSC32944 | Ebola | Filovirus | phenolic | alkaloid | virus | Influenza Virus | NSC-32944 | Zika | Cephaeline

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相关库: HIF-1 Signaling Pathway Compound Library | ReFRAME Related Library | Tobacco Monomer Library | Epigenetics Compound Library | Natural Product Library for HTS | NO PAINS Compound Library | Anti-Viral Compound Library | Anti-infective Natural Product Library | Bioactive Compound Library | Natural Product Library

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