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Biological Activity for Pladienolide B
Pladienolide B is a mRNA splicing inhibitor that decreases splicing capacity up to 75% in vitro. Pladienolide B directly targets splicesome-associated 130 (SAP130), inhibits splicing factor 3B subunit (SF3B1) and impairs U2 small nuclear ribonucleoprotein (U2 snRNP) interaction with pre-mRNA. Pladienolide B arrests the cell cycle in G1 and G2/M phases and displays antitumor activity against gastric cancer cells (IC50 values are 1.6-4.9 nM). Cell permeable and active in vivo.
Technical Data for Pladienolide B
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Pladienolide B
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Pladienolide B
The following data is based on the product molecular weight 536.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.02 mM||93.16 mL||465.81 mL||931.62 mL|
|0.1 mM||18.63 mL||93.16 mL||186.32 mL|
|0.2 mM||9.32 mL||46.58 mL||93.16 mL|
|1 mM||1.86 mL||9.32 mL||18.63 mL|
References for Pladienolide B
References are publications that support the biological activity of the product.
Lee et al (2016) Therapeutic targeting of splicing in cancer. Nature Medicine 22 976
Pederiva et al (2016) Splicing controls the ubiquitin response during DNA double-strand break repair. Cell Death Differ. 23 1648 PMID: 27315300
Sato et al (2014) High antitumor activity of pladienolide B and its derivative in gastric cancer. Cancer Sci. 105 110 PMID: 24635824
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Keywords: Pladienolide B, Pladienolide B supplier, mRNA, splicing, inhibitors, inhibits, splicesome-associated, 130, SAP130, factor, 3B, subunit, SF3B1, U2, small, nuclear, ribonucleoprotein, snRNP, cell, cycle, antitumor, anticancer, permeable, active, in, vivo, DNA,, RNA, and, Protein, Synthesis, Cell, Cycle, Inhibitors, 6070, Tocris Bioscience
4 Citations for Pladienolide B
Citations are publications that use Tocris products. Selected citations for Pladienolide B include:
Kotake et al (2007) Splicing factor SF3b as a target of the antitumor natural product pladienolide. Nat.Chem.Biol. 3 570 PMID: 17643112
Crews et al (2016) RNA splicing modulation selectively impairs leukemia stem cell maintenance in secondary human AML. Cell stem cell 19 599 PMID: 27570067
Salton et al (2016) Small molecule modulators of pre-mRNA splicing in cancer therapy. Trends Mol.Med. 22 28 PMID: 26700537
Disney et al (2008) Short-circuiting RNA splicing. Nat.Chem.Biol. 4 723 PMID: 19008883
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Literature in this Area
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