MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 ranging from 70 to 150 nmol/L. MPT0B098 arrests cells in the G2A–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, MPT0B098 not only inhibited the expression levels of HIF-1α protein but also destabilized HIF-1α mRNA. The mechanism of causing unstable of HIF-1α mRNA by MPT0B098 is through decreasing RNA-binding protein, HuR, translocation from the nucleus to the cytoplasm. Notably, MPT0B098 effectively suppresses tumor growth and microvessel density of tumor specimens in vivo. Taken together, our results provide a novel mechanism of inhibiting HIF-1α of a microtubule inhibitor MPT0B098. MPT0B098 is a promising anticancer drug candidate with potential for the treatment of human malignancies. ( Mol Cancer Ther; 2013, 12(7); 1202A–12. References: Cheng YC, Liou JP, Kuo CC, Lai WY, Shih KH, Chang CY, Pan WY, Tseng JT, Chang JY. MPT0B098, a Novel Microtubule Inhibitor That Destabilizes the Hypoxia-Inducible Factor-1α mRNA through Decreasing Nuclear-Cytoplasmic Translocation of RNA-Binding Protein HuR. Mol Cancer Ther. 2013 Jul;12(7):1202-12. doi: 10.1158/1535-7163.MCT-12-0778. Epub 2013 Apr 25. PubMed PMID: 23619299.

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CAS：1254363-89-7