BI 2536是一种新型、强效的、高选择性PLK1抑制剂(IC50=0.83 nM),也可以抑制PLK2 (IC50=3.5 nM)和PLK3 (IC50= 9.0 nM)。BI 2536诱导细胞有丝分裂阻断,并诱导癌细胞凋亡,另外,还可以抑制裸鼠体内移植瘤生长,诱导肿瘤衰退。BI 2536作用于AML细胞表现出强效的抗增殖作用。
The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15. [2]. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18...
PLK1抑制剂(BI 2536)755038-02-9Polo-like Kinase Inhibitor IVBI 2536, 10 mM in DMSOBI-2536 Plk1 inhibitor potent ATP-competitiveBI 2536 USP/EP/BP(R)-4-((8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxy-...
BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM, BI2536 shows 4- and 11-fold greater selectivity against Plk2 and Plk3; BI2536 also is a BRD4 inhibitor(IC50= 25 nM). BI 2536 blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 ...
BI2536是一种有效的选择性的Plk1抑制剂,IC50为0.83nM,也有效抑制BRD4,IC50为25nM。注:本品仅可用于科研实验,严禁用于临床医疗及其他用途!CAS号:755038-02-9纯度:99.19%分子式:C28H39N7O3分子量:521.65结构式:储存条件:-20℃,有效期2年,溶入溶剂后-20℃请尽量在一个月内使用。相关搜索:Plk1抑制剂(BI 2536...
BI 2536是一种有效的Plk1抑制剂,IC50为0.83 nM,比作用于Plk2和Plk3选择性分别高4和11倍。A Plk inhibitor with efficacy against 32 cancer cell lines. BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3.A Plk inhibitor ...
A selective inhibitor of Plk1 (IC50 = 0.83 nM); induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice; also an inhibitor of BRD4 (IC50 = 25 nM) 产品形式
BI 2536 is a small molecule inhibitor of mammalian polo-like kinases (PLKs) with a strong selectivity for PLK1 (IC50 = 0.83 nM) (1). PLK1 is important in regulating mitosis and is often overexpressed in cancers, contributing to excessive cell proliferation and loss of key checkpoint functions...
BI 2536 是PLK1和BRD4的双抑制剂,IC50分别为 0.83 和 25 nM。BI-2536 抑制 IFNB (IFN-β,干扰素 β) 基因转录。 BI 2536Chemical Structure CAS No. :755038-02-9 *Please selectQuantitybefore adding items. 生物活性 BI 2536 is a dualPLK1andBRD4inhibitor withIC50s of 0.83 and 25 nM, respectively...
The Plk1 inhibitor BI_2536 was well tolerated and showed antitumor activity in the first clinical trials enrolling patients with advanced solid tumors and refractory or relapsed acute myeloid leukemia.doi:10.1007/978-3-642-01222-8_15R Wäsch...