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(xì)胞性白血病(AML)中異常激活。它是一種細(xì)胞滲透性抑制劑,可降低AML細(xì)胞的集落形成能力(IC 50 200 nM),對(duì)正常造血祖細(xì)胞的細(xì)胞毒性作用極小。KP 372 -1還被證明可以抑制甲狀腺癌細(xì)胞和膠質(zhì)母細(xì)胞瘤的細(xì)胞增殖并誘導(dǎo)細(xì)胞凋亡。以區(qū)域異構(gòu)體的1:1混合物形式提供。參考資料由Bioz提供技術(shù)支持更多詳情請(qǐng)參閱Bioz 1)M。Mandal等人,“Akt抑制劑KP 372 -1抑制Akt活性和細(xì)胞增殖并誘導(dǎo)甲狀腺癌細(xì)胞凋亡”Br. J. Cancer 2005 92 1899-1905.2)Z. Zeng et al“Small-Molecule KP 372 -1同時(shí)抑制PDK 1/AKT和Fms樣酪氨酸激酶3信號(hào)傳導(dǎo)誘導(dǎo)急性髓細(xì)胞性白血病的線粒體功能障礙和細(xì)胞凋亡。“Cancer Res. 2006 66 3737-3746.
產(chǎn)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.