- Mps1-IN-2
AZ3146Mps1 inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Description | AZ3146 is a selective inhibitor of Mps1 with IC50 of ~35 nM. | |||||
Targets | Mps1 | |||||
IC50 | ~35 nM |
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Cas No. | 1124329-14-1 | SDF | Download SDF |
Synonyms | AZ 3146; AZ-3146 | ||
Chemical Name | 9-cyclopentyl-2-[2-methoxy-4-(1-methylpiperidin-4-yl)oxyanilino]-7-methylpurin-8-one | ||
Canonical SMILES | CN1CCC(CC1)OC2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCCC5)OC | ||
Formula | C24H32N6O3 | M.Wt | 452.55 |
Solubility | ≥15.3mg/mL in Ethanol | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
AZ3146 is a potent and selective Monopolar Spindle 1 (Mps1) kinase inhibitor with IC50 value of 35 nM. AZ3146 acts by interfering with chromosome alignment and overriding the spindle assembly checkpoint.
MPS1 protein kinases play important roles in different steps in mitosis including chromosome attachment and functions at the centrosomes. Additionally, they are also involved in regulation of development and in multiple signaling pathways after mitosis.
In cellular culture, if Mps1 is inhibited by AZ3146 before mitotic entry, this inhibition abloshed the subsequent recruitment of Mad1 and Mad2 to kinetochores. However, if cells were treated with AZ3146 after mitotic entry, the Mad1-C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. , AZ3146 interferes with chromosome alignment and overrides spindle assembly checkpoint1.
Regarding the effect of AZ3146 administration in vivo, the evidence should be provided by performing the study in human or mice or other animal models.
Reference:1. Hewitt L, Tighe A, Santaguida S, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. The Journal of cell biology.2010;190(1):25-34.
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(2)荧光标记法 : 使用二乙酸荧光素(FDP)、碘化丙啶(PI)或异硫氰酸荧光素钠标记的荧光染料与细胞共孵育,用流式细胞仪检测荧光染色阳性细胞的比率。此法其实是(1)法的“荧光”版,但其在灵敏性和准确性方面明显要优于后者。
(3)硝酸镧(La)示踪法: 在正常的生物组织中镧微粒可沉积于细胞间隙,但不能穿过具有1~ 2nm 微小间隙的细胞膜性结构(包括细胞膜和细胞器膜),也不能穿过细胞间的紧密连接。在膜性结构通透性增高时, 镧微粒则可进入细胞、细胞器和紧密连接内, 并在电镜下显示, 镧盐标记技术被认为是一种有效的监测细胞膜通透性变化的标记技术。
(4)LDH释放法: 在正常情况下,细胞内大分子物质LDH 是不能通过细胞膜的, 但在细胞膜受损伤而通透性增加时,可通过受损的细胞膜释放出来。LDH 能较好地反映细胞膜损伤程度。类似的还有检测细胞外K+的漏出率等。
有几个疑问
1:荧光标记到细胞是标记到细胞表面还是细胞质内?
2:荧光应该随着细胞的分化和增殖逐渐消失?是不是分化增殖越快,荧光消失速度越快?
3:有哪些容易操作,成本便宜的荧光物质?
谢谢各位战友
比如你用的CD1a-FITC(如果是鼠单抗IgG1,那对照抗体就要用相同物种的非特异性IgG1-FITC)。注意浓度要相同。一般提供抗体的公司BD,santa cruz等有提供的。其他就按照说明书的推荐浓度和孵育时间。