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 ActivityPladienolide 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.
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Splicing controls the ubiquitin response during DNA double-strand break repair.
Pederiva C, Bohm S, Julner A, Farnebo M.
Cell Death Differ
Therapeutic targeting of splicing in cancer.
Lee et al.
Nature Medicine, 2016;22:976
High antitumor activity of pladienolide B and its derivative in gastric cancer.
Sato et al.
Cancer Sci., 2014;105:110
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
Small molecule modulators of pre-mRNA splicing in cancer therapy.
Authors: Salton Et al.
Trends Mol.Med. 2016;22:28
RNA splicing modulation selectively impairs leukemia stem cell maintenance in secondary human AML.
Authors: Crews Et al.
Cell stem cell 2016;19:599
Short-circuiting RNA splicing.
Authors: Disney Et al.
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
Authors: Kotake Et al.
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