CLK1-IN-1|cas:2123491-32-5|西域试剂

CLK1-IN-1,99.05%

产品编号：Bellancom-103082| CAS NO：2123491-32-5| 分子式：C₂₄H₁₆FN₅O| 分子量：409.42

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货号	价格	库存与货期
Bellancom-103082	￥3500.00	杭州北京（现货）
Bellancom-103082	￥6000.00	杭州北京（现货）
Bellancom-103082	￥12500.00	杭州北京（现货）

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CLK1-IN-1

产品介绍

CLK1-IN-1 是一个有效的、Cdc2-like 激酶 (CLK1) 的选择性抑制剂，其 IC₅₀ 值为 2 nM。

生物活性

CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC₅₀ of 2 nM.

体外研究

CLK1 is the most potently inhibited kinase (IC₅₀: 2 nM). In addition to CLK1, only two kinases have an IC₅₀ value less than 100 nM, namely CLK2 (IC₅₀: 31 nM) and CLK4 (IC₅₀: 8 nM), DYRK1A is the strongest off-target. The ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

APAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (61.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4425 mL	12.2124 mL	24.4248 mL
5 mM	0.4885 mL	2.4425 mL	4.8850 mL
10 mM	0.2442 mL	1.2212 mL	2.4425 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。-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 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。