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Pladienolide B is a mRNA splicing inhibitor, exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B decreases splicing capacity up to 75% in vitro. Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B induces apoptosis. 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 cell cycle in G1 and G2/M phases. Pladienolide B displays antitumor activity against gastric cancer cells (IC50 values are 1.6-4.9 nM). Pladienolide B is cell permeable and active in vivo.
Pladienolides B can be dissolved in DMSO for in vitro use.
For in vivo study, pladienolides B were dissolved at appropriate concentrations in 3.5% DMSO and 6.5% Tween 80 in 5% glucose solution.
| Molecular Weight | 536.7 |
| Formula | C30H48O8 |
| CAS Number | 445493-23-2 |
| Solubility (25°C) | DMSO |
| Storage | -20°C, sealed |
[1] Bowery. TiPS. GABAB receptors and their significance in mammalian pharmacology.
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