Pladienolide B

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Cat.No. 6070 - Pladienolide B | C30H48O8 | CAS No. 445493-23-2
Description: mRNA splicing inhibitor; antitumor
Chemical Name: (4R,7R,8S,9E,11S,12S)-8-(Acetyloxy)-4,7-dihydroxy-12-[(1E,3E,5S)-6-[(2R,3R)-3-[(1R,2S)-2-hydroxy-1-methylbutyl]-2-oxiranyl]-1,5-dimethyl-1,3-hexadien-1-yl]-7,11-dimethyloxacyclododec-9-en-2-one
Purity: ≥95% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

mRNA splicing inhibitor; decreases splicing capacity up to 75% in vitro. Directly targets splicesome-associated 130 (SAP130), inhibits splicing factor 3B subunit (SF3B1) and impairs U2 small nuclear ribonucleoprotein (U2 snRNP) interaction with pre-mRNA. Arrests cell cycle in G1 and G2/M phases. Displays antitumor activity against gastric cancer cells (IC50 values are 1.6-4.9 nM). Cell permeable and active in vivo.

Technical Data

M. Wt 536.7
Formula C30H48O8
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 445493-23-2
PubChem ID 90909513
InChI Key SDOUORKJIJYJNW-UHFFFAOYSA-N
Smiles C[C@@H](/C=C/[C@H](OC(C)=O)[C@](C)(O)CC[C@@H](O)C1)[C@@H](/C(C)=C/C=C/[C@@H](C)C[C@@H]2[C@@H]([C@H](C)[C@@H](O)CC)O2)OC1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 1 2

Preparing Stock Solutions

The following data is based on the product molecular weight 536.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.86 mL 9.32 mL 18.63 mL
5 mM 0.37 mL 1.86 mL 3.73 mL
10 mM 0.19 mL 0.93 mL 1.86 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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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View all DNA, RNA and Protein Synthesis Inhibitors

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:

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

Kotake et al (2007) Splicing factor SF3b as a target of the antitumor natural product pladienolide. Nat.Chem.Biol. 3 570 PMID: 17643112


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Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis