Pladienolide B

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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)
Citations (4)
Literature (3)

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

M. Wt 536.7
Formula C30H48O8
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 445493-23-2
PubChem ID 90909513
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.

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
DMSO 1 2

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Pladienolide B

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for Pladienolide B, please let us know.

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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:

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

Do you know of a great paper that uses Pladienolide B from Tocris? Please let us know.

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Literature in this Area

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