货号:A723868
同义名:
Passenger Proteins Transport Inhibitor
Paprotrain is reversible, non-ATP competitive inhibitor of mitotic kinesin-like protein 2 (MKLP-2) with Ki of 3.4 μM.
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描述 | Mitotic kinesin‐like protein 2 (MKLP‐2), a member of the kinesin‐6 family, is essential for cytokinesis. Paprotrain is a reversible inhibitor of MKLP‐2 uncompetitive with ATP (Ki = 3.4 ± 0.1 μM ) and noncompetitive with microtubules (MTs; Ki = 1.6 ± 0.1 μM ). It is specific for MKLP‐2 as it does not inhibit other members of the kinesin superfamily. IC50 values were (1.35 ± 0.2) μM in basal and (0.83 ± 0.1) μM in MT‐stimulated ATPase assays. After 24 h of treatment with paprotrain (10–50 μM ), a significant number of cells were in apoptosis, confirmed by immunodetection of cleaved poly(ADP‐ribose) polymerase (PARP) and activated caspase 3. Paprotrain (50 μM; 8 h) induced binucleated cells and impeded the relocation of the CPC (the chromosome passenger protein complex) from the inner centromeres to the central spindle during anaphase. In proliferation assays, paprotrain inhibited growth with EC50 values between 7.6 and 22 μM. Moreover, after treatment with paprotrain the majority of metaphase spindles (70 ± 10 % of total metaphase cells) had misaligned chromosomes. Higher concentrations of paprotrain (50 μM ) increased the percentage of multipolar spindles at the expense of normal bipolar spindles (14 ± 3 % of total metaphase cells at 50 μM versus 6 ± 1.6 % at 20 μM)[1]. Furthermore, the rate of polar body extrusion in oocytes treated with 50 µM Paprotrain was significantly reduced to 42.07 ± 7.41%[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
4.08mL 0.82mL 0.41mL |
20.38mL 4.08mL 2.04mL |
40.77mL 8.15mL 4.08mL |
CAS号 | 57046-73-8 |
分子式 | C16H11N3 |
分子量 | 245.279 |
别名 | Passenger Proteins Transport Inhibitor |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 105 mg/mL(428.08 mM),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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |