PARP1-IN-2 (化合物 11g) 是一种有效的可透过血脑屏障的PARP1抑制剂,其IC50值为 149 nM。PARP1-IN-2 对人肺腺癌上皮细胞系 A549 具有显著的抗增殖活性。PARP1-IN-2 可诱导 A549 细胞凋亡。
生物活性 | PARP-1-IN-2 (compound 11g) is a potent and BBB-penetratedPARP1inhibitor, with anIC50of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cellsapoptosis[1]. |
IC50& Target | PARP-1 149 ± 11.0 nM (IC50) | Caspase-3 | Caspase-9 |
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体外研究 (In Vitro) | PARP-1-IN-2 (compound 11g) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells[1]. PARP-1-IN-2 (0-10 μM, 24 h) decreases the expression of pro-caspase-3 and phosphorylated AKT, increases the expression of caspase-3, caspase-9 protein and the cleaved PARP-1[1].
Cell Proliferation Assay Cell Line: | A549, HFF cells[1] | Concentration: | 0, 0.1, 1, 10 μM | Incubation Time: | 24, 48 h | Result: | Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells. |
Western Blot Analysis Cell Line: | A549 cells[1] | Concentration: | 0, 0.1, 1, 10 μM | Incubation Time: | 24 h | Result: | Reduced expression of pro-caspase-3 and phosphorylated AKT, significantly increased the expression of caspase-3 and caspase-9 protein, and enhanced expression of the cleaved PARP-1. |
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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 : 83.33 mg/mL(196.40 mM;Need ultrasonic) 配制储备液 1 mM | 2.3569 mL | 11.7847 mL | 23.5693 mL | 5 mM | 0.4714 mL | 2.3569 mL | 4.7139 mL | 10 mM | 0.2357 mL | 1.1785 mL | 2.3569 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.90 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.90 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 20.8 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.90 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 20.8 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。 |