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Pladienolide B

Catalog #: 6070
10 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6070/500U
Pladienolide B | CAS No. 445493-23-2 | DNA, RNA and Protein Synthesis Inhibitors
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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%

Product Details
Citations (10)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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). Transient treatment with pladienolide B can reprogram pluripotent hESCs into a distinct type of zigotic genome activation (ZGA)-like cells (ZLCs). 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:

10 Citations: Showing 1 - 10

  1. Capturing totipotency in human cells through spliceosomal repression.
    Authors: Li Et al.
    Cell  2024;187:3284
  2. Highly efficient generation of blastocyst-like structures from spliceosomes-repressed mouse totipotent blastomere-like cells.
    Authors: Wenjing Et al.
    Sci China Life Sci  2023;66:423-435
  3. 8C-like cells capture the human zygotic genome activation program in vitro.
    Authors: Wolf Et al.
    Cell Stem Cell  2022;29:449-459.e6
  4. Modulation of SF3B1 in the pre-mRNA spliceosome induces a RIG-I-dependent type I IFN response.
    Authors: Frank Et al.
    J Biol Chem  2021;297:101277
  5. Pharmacologic modulation of RNA splicing enhances anti-tumor immunity.
    Authors: Jing Et al.
    Cell  2021;184:4032-4047.e31
  6. ATR Protects the Genome against R Loops through a MUS81-Triggered Feedback Loop.
    Authors: Lee Et al.
    Mol Cell  2020;77:514-527.e4
  7. Small molecule modulators of pre-mRNA splicing in cancer therapy.
    Authors: Salton Et al.
    Trends Mol.Med.  2016;22:28
  8. RNA splicing modulation selectively impairs leukemia stem cell maintenance in secondary human AML.
    Authors: Crews Et al.
    Cell stem cell  2016;19:599
  9. Short-circuiting RNA splicing.
    Authors: Disney Et al.
    Nat.Chem.Biol.  2008;4:723
  10. 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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