Pentachloropseudilin (Antibiotic A 15104 Y; PClP) 是一种可逆的、变构有效的肌球蛋白 (Myo1s) 抑制剂，对 Myo1s 的IC50范围为 1 至 5 μM，对于 2 类和 5 类肌球蛋白，IC50范围 >90 μM。Pentachloropseudilin 是转化生长因子-β(TGF-β)刺激的信号传导的有效抑制剂，对 TGF-β 的IC50值为 0.1-0.2 μM。
| 生物活性 | Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor ofMyo1s(class 1 myosins) withIC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor oftransforming growth factor-β(TGF-β)-stimulated signaling, with anIC50of 0.1 to 0.2 μM for TGF-β[1][2]. |
体外研究
(In Vitro) | Pentachloropseudilin (PClP) inhibits TGF-β-stimulated Smad2/3 phosphorylation and plasminogen activator inhibitor-1 (PAI-1) promoter activation with an IC50of 0.1 μM in target cells (A549, HepG2, and Mv1Lu cells)[1].
Pentachloropseudilin attenuates TGF-β-stimulated expression of vimentin, N-cadherin, and fibronectin and, thus, blocks TGF-β-induced epithelial to mesenchymal transition (EMT) in these cells. Pentachloropseudilin (0.05 to 1 μΜ; 0-6 hours) pretreatment inhibits TGF-β-mediated (50 or 100 pM) increases in p-Smad2/3 expression to 47% (Mv1Lu) and 79% (A549), respectively[1].
Pentachloropseudilin (0.2 μM) suppresses TGF-β-stimulated cellular responses by attenuating cell-surface expression of the type II TGF-β receptor through accelerating caveolae-mediated internalization followed by primarily lysosome-dependent degradation of the receptor, as demonstrated by sucrose density gradient analysis and immune fluorescence staining[1].
Pentachloropseudilin (200 μM; 24 hours) exhibits and altered cell viability in HUVECs[2].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(301.74 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.0174 mL | 15.0871 mL | 30.1741 mL | | 5 mM | 0.6035 mL | 3.0174 mL | 6.0348 mL | | 10 mM | 0.3017 mL | 1.5087 mL | 3.0174 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。-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%corn oil Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.54 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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