Paprotrain - CAS:57046-73-8

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Paprotrain

目录号 : KM9599 CAS No. : 57046-73-8 纯度 : 98%

Data Sheet 产品使用指南

Paprotrain是可渗透细胞的kinesin MKLP-2 的抑制剂，抑制 MKLP-2 的 ATPase 活性，IC₅₀ 值为 1.35 μM，K_i 值为 3.36 μM，同时对 DYRK1A 有中等的抑制作用，IC₅₀值为 5.5 μM。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC₅₀ of 1.35 μM and a K_i of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC₅₀ of 5.5 μM.

体外研究

Paprotrain has been screened on a panel of CNS kinases. While inactive (IC₅₀ >10 μM) on CDK5 and GSK3, it has shown a moderate activity on DYRK1A (IC₅₀=5.5 μM). Time-lapse microscopy shows that disrupting MKlp2 expression with paprotrain results in polar body extrusion failure. This could be rescued after rescuing oocytes from paprotrain in fresh medium. Cell cycle analysis shows that most oocytes are arrested at metaphase I or telophase I. However, oocyte spindle structure and chromosome alignment are not disrupted after the inhibition of MKlp2 by paprotrain. Paprotrain-treated porcine oocytes suffer failure of nuclear maturation. The number of oocytes arrested at early MI stage increase in a dose-dependent manner after KIF20A activity inhibition, while the percentage of oocytes that reach ATI and MII stages decrease after treatment.

分子式

C₁₆H₁₁N₃

分子量

245.28

CAS号

57046-73-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (407.70 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0770 mL	20.3849 mL	40.7697 mL
5 mM	0.8154 mL	4.0770 mL	8.1539 mL
10 mM	0.4077 mL	2.0385 mL	4.0770 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。