Pladienolide B

Catalog # Availability Size / Price Qty
6070/500U
Pladienolide B | CAS No. 445493-23-2 | DNA, RNA and Protein Synthesis Inhibitors
1 Image
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%

Product Details
Citations (4)
Reviews

Biological Activity

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

M.Wt:
536.7
Formula:
C30H48O8
Solubility:
Soluble to 1 mg/ml in DMSO
Purity:
≥95%
Storage:
Store at -20°C
CAS No:
445493-23-2

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.

Background References

  1. Splicing controls the ubiquitin response during DNA double-strand break repair.
    Pederiva C, Bohm S, Julner A, Farnebo M.
    Cell Death Differ.
  2. Therapeutic targeting of splicing in cancer.
    Lee et al.
    Nature Medicine, 2016;22:976
  3. High antitumor activity of pladienolide B and its derivative in gastric cancer.
    Sato et al.
    Cancer Sci., 2014;105:110

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Citations for Pladienolide B

The citations listed below are publications that use Tocris products. Selected citations for Pladienolide B include:

4 Citations: Showing 1 - 4

  1. Small molecule modulators of pre-mRNA splicing in cancer therapy.
    Authors: Salton Et al.
    Trends Mol.Med.  2016;22:28
  2. RNA splicing modulation selectively impairs leukemia stem cell maintenance in secondary human AML.
    Authors: Crews Et al.
    Cell stem cell  2016;19:599
  3. Short-circuiting RNA splicing.
    Authors: Disney Et al.
    Nat.Chem.Biol.  2008;4:723
  4. Splicing factor SF3b as a target of the antitumor natural product pladienolide.
    Authors: Kotake Et al.
    Nat.Chem.Biol.  2007;3:570

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