Pentachloropseudilin
规格
Cas Number | 69640-38-6 |
规格或纯度 | ≥98% |
纯度 | ≥98% |
包装 | 5mg |
产品信息
品牌 | 阿拉丁 |
溶解性 | DMSO : 100 mg/mL (301.74 mM; Need ultrasonic) |
过滤标签 | TGF-β Receptor,Myosin,TGF-beta/Smad,Cytoskeleton |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | 五氯伪素(抗生素 A 15104 Y;PClP)是 Myo1s(1 类肌球蛋白)的可逆异构强效抑制剂,对哺乳动物 1 类肌球蛋白的 IC 50 s 范围为 1 至 5 μM,对 2 类和 5 类肌球蛋白的 IC 50 s 范围大于 90 μM。五氯 |
英文描述 |
Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC 50 s 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 of transforming growth factor-β (TGF-β) -stimulated signaling, with an IC 50 of 0.1 to 0.2 μM for TGF-β. In Vitro Pentachloropseudilin (PClP) inhibits TGF-β-stimulated Smad2/3 phosphorylation and plasminogen activator inhibitor-1 (PAI-1) promoter activation with an IC 50 of 0.1 μM in target cells (A549, HepG2, and Mv1Lu cells). 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. 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. Pentachloropseudilin (200 μM; 24 hours) exhibits and altered cell viability in HUVECs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid |