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CAS No.: 57046-73-8

Paprotrain Catalog No. CSN25340

Synonyms: 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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技术信息

生物活性

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 (K_i = 3.4 ± 0.1 μM ) and noncompetitive with microtubules (MTs; K_i = 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].
参考文献

[1] Tcherniuk S, Skoufias DA, Labriere C, et al. Relocation of Aurora B and survivin from centromeres to the central spindle impaired by a kinesin-specific MKLP-2 inhibitor. Angew Chem Int Ed Engl. 2010;49(44):8228-8231
[2] Zhang Y, Liu J, Peng X, et al. KIF20A regulates porcine oocyte maturation and early embryo development. PLoS One. 2014;9(7):e102898. Published 2014 Jul 18

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0770 mL
- 20.3850 mL
- 40.7700 mL
- 5 mM
- 0.8154 mL
- 4.0770 mL
- 8.1540 mL
- 10 mM
- 0.4077 mL
- 2.0385 mL
- 4.0770 mL

技术信息

CAS号

57046-73-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H11N3

运输

蓝冰

分子量

245.28

别名

Passenger Proteins Transport Inhibitor

溶解度

DMSO	98.0 mg/mL (399.5 mM)

动物实验配方

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