KP 372 -1直接抑制Akt PDK 1和Flt 3（Fms樣酪氨酸激酶3）的激酶活性，這些激酶在急性髓細胞性白血?。ˋML）中異常激活。它是一種細胞滲透性抑制劑，可降低AML細胞的集落形成能力（IC 50 200 nM），對正常造血祖細胞的細胞毒性作用極小。KP 372 -1還被證明可以抑制甲狀腺癌細胞和膠質母細胞瘤的細胞增殖并誘導細胞凋亡。以區域異構體的1：1混合物形式提供。參考資料由Bioz提供技術支持更多詳情請參閱Bioz 1）M。Mandal等人，“Akt抑制劑KP 372 -1抑制Akt活性和細胞增殖并誘導甲狀腺癌細胞凋亡”Br. J. Cancer 2005 92 1899-1905.2）Z. Zeng et al“Small-Molecule KP 372 -1同時抑制PDK 1/AKT和Fms樣酪氨酸激酶3信號傳導誘導急性髓細胞性白血病的線粒體功能障礙和細胞凋亡?！癈ancer Res. 2006 66 3737-3746.
產品描述
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.
