KP 372 -1直接抑制Akt PDK 1和Flt 3（Fms样酪氨酸激酶3）的激酶活性，这些激酶在急性髓细胞性白血病（AML）中异常激活。它是一种细胞渗透性抑制剂，可降低AML细胞的集落形成能力（IC 50 200 nM），对正常造血祖细胞的细胞毒性作用极小。KP 372 -1还被证明可以抑制甲状腺癌细胞和胶质母细胞瘤的细胞增殖并诱导细胞凋亡。以区域异构体的1：1混合物形式提供。参考资料由Bioz提供技术支持更多详情请参阅Bioz 1）M。Mandal等人，“Akt抑制剂KP 372 -1抑制Akt活性和细胞增殖并诱导甲状腺癌细胞凋亡”Br. J. Cancer 2005 92 1899-1905.2）Z. Zeng et al“Small-Molecule KP 372 -1同时抑制PDK 1/AKT和Fms样酪氨酸激酶3信号传导诱导急性髓细胞性白血病的线粒体功能障碍和细胞凋亡。“Cancer Res. 2006 66 3737-3746.
产品描述
KP372-1 directly inhibits the kinase activities of Akt PDK1 and Flt3 (Fms-like tyrosine kinase 3) which are aberrantly activated in acute myelogenous leukemia (AML). It is a cell permeant inhibitor that decreases the colony-forming ability of AML cells (IC50 < 200 nM) with minimal cytoxic effects on normal hematopoietic progenitor cells. KP372-1 has also been shown to suppress cell proliferation and induce apoptosis in thyroid cancer cells and gliobastoma. Provided as a 1:1 mixture of regioisomers.References Powered by Bioz See more details on Bioz1) M. Mandal et al. "The Akt Inhibitor KP372-1 Suppresses Akt Activity and Cell Proliferation and Induces Apoptosis in Thyroid Cancer Cells" Br. J. Cancer 2005 92 1899-1905.2) Z. Zeng et al "Simultaneous Inhibition of PDK1/AKT and Fms-Like Tyrosine Kinase 3 Signaling by a Small-Molecule KP372-1 Induces Mitochondrial Dysfunction and Apoptosis in Acute Myelogenous Leukemia." Cancer Res. 2006 66 3737-3746.
