Catalog Number: 6070
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
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
  • 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. All Tocris products are intended for laboratory research use only.
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
Citations:

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

4 Citations: Showing 1 - 4
Filter your results:

  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
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

or select another batch: 

Feedback

Customer Information