Phenol,2,4-dibromo-6-(3,4,5-tribromo-1H-pyrrol-2-yl)-

Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and cancer[1].

Research Areas >> Cancer

Pentabromopseudilin (PBrP) (0.01-1 μM, 6 h) 可防止 TGF-β 诱导的 Smad 蛋白磷酸化和核转位[1]。 PBrP (0.5 μM, 6 h) 抑制 TGF-β 刺激的转录反应[1]。 PBrP (0-1 μM, 6 h) 抑制 A549 细胞中 TGF-β 诱导的 EMT[1]。 PBrP (0.2 μM, 20 h) 抑制 TGF-β 诱导的细胞迁移[1]。 PBrP (0.01-1⟩μM, 6 h) 通过增强 TβRII 的降解来阻断 TGF-β 信号传导[1]。 PBrP (0.5μM, 0, 1, 3 h) 通过细胞膜穴样内陷增强 TβRII 的降解来阻断 TGF-β 信号传导[1]。 Western Blot Analysis[1] Cell Line: Mv1Lu, A549, Clone 9 and HepG2 cells Concentration: 0.01-1 μM (Mv1Lu, A549, Clone 9 and HepG2 cells); 0.5 μM (Mv1Lu, A549 and HepG2 cells) Incubation Time: 6 h (Mv1Lu, A549, Clone 9 and HepG2 cells); 0.5, 1, 2, 4, 6 h (Mv1Lu, A549 and HepG2 cells) Result: Suppressed the TGF-β-stimulated Smad2/3 phosphorylation in a dose-dependent manner in these cell lines. Prevented TGF-β induced the nuclear translocation of Smad2/3 and PBrP alone did not alter the localisation of Smad proteins. Immunofluorescence[1] Cell Line: A549 cells Concentration: 0.2 μM Incubation Time: 6 h Result: Abolished TGF-β-induced Smad2/3 nuclear translocation. Cell Migration Assay [1] Cell Line: A549 cells Concentration: 0.2 μM Incubation Time: 20 h Result: Suppressed TGF-β-stimulated cell migration and did not close the wound.

[1]. Shih-Wei W, et al. Pentabromopseudilin: a myosin V inhibitor suppresses TGF-β activity by recruiting the type II TGF-β receptor to lysosomal degradation. J Enzyme Inhib Med Chem. 2018;33(1):920-935.