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Pladienolide B

Cat. No. 6070 10 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： mRNA splicing inhibitor; antitumor
化学名： (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
纯度： ≥95% (HPLC)
说明书
引用文献 (10)
评论
文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

技术数据 for Pladienolide B

分子量 536.7
公式 C30H48O8
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Pladienolide B

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 1 2

制备储备液 for Pladienolide B

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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产品说明书 for Pladienolide B

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Pladienolide B

参考文献是支持产品生物活性的出版物。

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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关键词: 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 篇 Pladienolide B 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Pladienolide B 的部分引用包括：

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

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

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

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

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