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Pladienolide B

Cat. No. 6070 10 Citations Submit a Review Datasheet / COA / SDS
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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% (HPLC)
Datasheet
Citations (10)
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Pladienolide B

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 for Pladienolide B

M. Wt 536.7
Formula C30H48O8
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 445493-23-2
PubChem ID 90909513
InChI Key SDOUORKJIJYJNW-UHFFFAOYSA-N
Smiles C[C@@H](/C=C/[C@H](OC(C)=O)[C@](C)(O)CC[C@@H](O)C1)[C@@H](/C(C)=C/C=C/[C@@H](C)C[C@@H]2[C@@H]([C@H](C)[C@@H](O)CC)O2)OC1=O

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.

Solubility Data for Pladienolide B

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 1 2

Preparing Stock Solutions for Pladienolide B

The following data is based on the product molecular weight 536.7. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.02 mM 93.16 mL 465.81 mL 931.62 mL
0.1 mM 18.63 mL 93.16 mL 186.32 mL
0.2 mM 9.32 mL 46.58 mL 93.16 mL
1 mM 1.86 mL 9.32 mL 18.63 mL

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Product Datasheets for Pladienolide B

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for Pladienolide B

References are publications that support the biological activity of the product.

Lee et al (2016) Therapeutic targeting of splicing in cancer. Nature Medicine 22 976

Pederiva et al (2016) Splicing controls the ubiquitin response during DNA double-strand break repair. Cell Death Differ. 23 1648 PMID: 27315300

Sato et al (2014) High antitumor activity of pladienolide B and its derivative in gastric cancer. Cancer Sci. 105 110 PMID: 24635824

Li et al (2024) Capturing totipotency in human cells through spliceosomal repression. Cell 187 3284 PMID: 38843832

If you know of a relevant reference for Pladienolide B, please let us know.

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Keywords: Pladienolide B, Pladienolide B supplier, mRNA, splicing, inhibitors, inhibits, splicesome-associated, 130, SAP130, factor, 3B, subunit, SF3B1, U2, small, nuclear, ribonucleoprotein, snRNP, cell, cycle, antitumor, anticancer, permeable, active, in, vivo, stem, reprogramming, zigotic, genome, activation, DNA,, RNA, and, Protein, Synthesis, Cell, Cycle, Inhibitors, Stem, Reprogramming, 6070, Tocris Bioscience

10 Citations for Pladienolide B

Citations are publications that use Tocris products. Selected citations for Pladienolide B include:

Lee et al (2020) ATR Protects the Genome against R Loops through a MUS81-Triggered Feedback Loop. Mol Cell 77 514-527.e4 PMID: 31708417

Frank et al (2021) Modulation of SF3B1 in the pre-mRNA spliceosome induces a RIG-I-dependent type I IFN response. J Biol Chem 297 101277 PMID: 34619148

Jing et al (2021) Pharmacologic modulation of RNA splicing enhances anti-tumor immunity. Cell 184 4032-4047.e31 PMID: 34171309

Disney et al (2008) Short-circuiting RNA splicing. Nat.Chem.Biol. 4 723 PMID: 19008883

Crews et al (2016) RNA splicing modulation selectively impairs leukemia stem cell maintenance in secondary human AML. Cell stem cell 19 599 PMID: 27570067

Salton et al (2016) Small molecule modulators of pre-mRNA splicing in cancer therapy. Trends Mol.Med. 22 28 PMID: 26700537

Wenjing et al (2023) Highly efficient generation of blastocyst-like structures from spliceosomes-repressed mouse totipotent blastomere-like cells. Sci China Life Sci 66 423-435 PMID: 36633710

Wolf et al (2022) 8C-like cells capture the human zygotic genome activation program in vitro. Cell Stem Cell 29 449-459.e6 PMID: 35216671

Li et al (2024) Capturing totipotency in human cells through spliceosomal repression. Cell 187 3284 PMID: 38843832

Kotake et al (2007) Splicing factor SF3b as a target of the antitumor natural product pladienolide. Nat.Chem.Biol. 3 570 PMID: 17643112

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Literature in this Area

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