3-IN-PP1 是一种蛋白激酶 D (PKD) 抑制剂。 3-IN-PP1 对 PKD1、PKD2 和 PKD3 具有有效广泛的 PKD 抑制活性,IC50值分别为 108、94 和 108 nM。3-IN-PP1 也是一种广谱抗癌剂,对多种肿瘤细胞的生长有抑制作用。3-IN-PP1 可用于癌症研究。
生物活性 | 3-IN-PP1 is aprotein kinase D (PKD)inhibitor. 3-IN-PP1 has potent pan-PKD inhibitory activity forPKD1,PKD2andPKD3withIC50values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research ofcancer[1]. |
IC50& Target[1] | PKD1 108 nM (IC50) | Cellular PKD2 94 nM (IC50) | PKD3 108 nM (IC50) |
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体外研究 (In Vitro) | 3-IN-PP1 has potent pan-PKD inhibitory activity for PKD1, PKD2 and PKD3 with IC50values of 108, 94 and 108 nM, respectively[1]. 3-IN-PP1 (5 μM, 0-114 h) displays potent anti-proliferative activity against PANC-1 cells[1]. 3-IN-PP1 (20 μM, 1 h) potently blocks PKD-dependent cortactin phosphorylation in PANC-1 cells[1]. 3-IN-PP1 has inhibition of different tumor cell growth with IC50values range from 1.6 to 39.2μM[1].
Cell Proliferation Assay[1] Cell Line: | PANC-1 cell | Concentration: | 5 μM | Incubation Time: | 0-114 h | Result: | Significantly inhibited PANC-1 cell proliferation after incubation for 96 and 144 hours. |
Western Blot Analysis[1] Cell Line: | PANC-1 cells | Concentration: | 20 μM | Incubation Time: | 1 h | Result: | Reduced cortactin phosphorylation in PANC-1 cells. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(326.40 mM;Need ultrasonic) 配制储备液 1 mM | 3.2640 mL | 16.3201 mL | 32.6403 mL | 5 mM | 0.6528 mL | 3.2640 mL | 6.5281 mL | 10 mM | 0.3264 mL | 1.6320 mL | 3.2640 mL |
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 (8.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.16 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.16 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.16 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.16 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。 *以上所有助溶剂都可在本网站选购。
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