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快速发货 顺丰冷链运输,1-2 天到达
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产品名称 | Kinesin ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SB-743921 HCl |
++++
KSP (P388 cells), IC50: 14.4 nM KSP, Ki: 0.07 nM |
99%+ | |||||||||||||||||
GSK-923295 |
++
CENP-E, Ki: 3.2 nM |
99%+ | |||||||||||||||||
Ispinesib |
+++
KSP (HsEg5), Ki app: 1.7 nM |
99%+ | |||||||||||||||||
AZ3146 |
+
Mps1, IC50: ~35 nM |
98+% | |||||||||||||||||
MPI-0479605 |
++
Mps1, IC50: 1.8 nM |
99%+ | |||||||||||||||||
BAY1217389 |
+++
Mps1, IC50: 0.63 nM |
98% | |||||||||||||||||
ARQ 621 | ✔ | 98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Monopolar spindle 1 (Mps1) is a spindle assembly checkpoint kinase that plays an essential role in the regulation of mitosis. AZ3146 inhibits human Mps1 with an IC50 value of 35 nM. In nocodazole-arrested Hela cells, AZ3146 at 1 – 30 μM inhibited the autophosphorylation of full-length Mps1. AZ3146 at 2 µM reduced the time for Hela cells to complete mitosis from 90 min to 32 min. Nearly 90% of AZ3146-treated Hela cells underwent abnormal mitoses with around 50% entering anaphase without aligning all the chromosomes and almost 30% exiting mitosis without chromosome segregation. AZ3146 at 2 µM also decreased the levels of Mad1 and Mad2 to 60% and 15%, respectively. The kinetochore recruitment of O-Mad2 in Hela cells was also blocked by at 2 µM AZ3146[3]. The exposure of GSK923295, an inhibitor targeting the mitotic kinesin Cenp-E, combined with 2 µM AZ3146 induced whole chromosome aneuploidies in cells without causing DNA damage and significant disruption to the spindle[4]. In AZ3146-resistent HCT116 cells created by long-term exposure of AZ3146, 24-hour incubation of 1 and 2 µM AZ3146 abolished the G1 and G2 - M peaks in the parental cell line and made them rapidly exit from mitosis[5]. |
作用机制 | AZ3146 might inhibit Mps1 by promoting its kinetochore localization[3]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human HCT116 cells | Function assay | Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132, IC50=0.72 μM | 24256217 | ||
human HCT116 cells | Growth inhibition assay | 72 h | Growth inhibition in human HCT116 cells after 72 hrs by MTT assay, GI50=1.2 μM | 24256217 | |
sf9 insect cells | Function assay | Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay, IC50=7 nM | 24256217 |
Dose | Mice: 50 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.21mL 0.44mL 0.22mL |
11.05mL 2.21mL 1.10mL |
22.10mL 4.42mL 2.21mL |
CAS号 | 1124329-14-1 |
分子式 | C24H32N6O3 |
分子量 | 452.549 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 105 mg/mL(232.02 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |