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Submit ReviewTriptolide
说明： Inhibits RNAPII-mediated transcription; antitumor, anti-inflammatory and immunosuppressive
化学名： (3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-Decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one
纯度： ≥98% (HPLC)
生物活性 for Triptolide
Triptolide inhibits DNA-dependent ATPase activity of XBP and induces inhibition of RNA polymerase II (RNAPII)-mediated transcription (IC50 = 200 nM). Selective for RNAPII over RNAPI and RNAPIII. Triptolide blocks RNA synthesis in HeLa cells (IC50 = 62 nM); exhibits potent antiproliferative activity in 60 cancer cell lines (average IC50 = 12 nM) and induces apoptosis by blocking TNF-α-mediated c-IAP1 and c-IAP2 induction. Also displays immunosuppressive and anti-inflammatory activity.
化合物库 for Triptolide
Triptolide is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Triptolide
| 分子量 | 360.4 |
| 公式 | C20H24O6 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 38748-32-2 |
| PubChem ID | 107985 |
| InChI Key | DFBIRQPKNDILPW-CIVMWXNOSA-N |
| Smiles | O=C1C2=C([C@@](C[C@H]5[C@]4(O5)[C@](O6)3[C@@H]6[C@H]7[C@](C(C)C)(O7)[C@H]4O)([H])[C@]3(C)CC2)CO1 |
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 Triptolide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 7.21 | 20 |
制备储备液 for Triptolide
以下数据基于产品分子量 360.4。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.87 mL | 69.37 mL | 138.73 mL |
| 1 mM | 2.77 mL | 13.87 mL | 27.75 mL |
| 2 mM | 1.39 mL | 6.94 mL | 13.87 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.77 mL |
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产品说明书 for Triptolide
参考文献 for Triptolide
参考文献是支持产品生物活性的出版物。
Qui et al (1999) Immunosuppressant PG490 (Triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T-cells and NF-κB transcriptional activation. J.Biol.Chem. 274 13443 PMID: 10224109
Lee et al (1999) PG490 (Triptolide) cooperates with tumor necrosis factor-α to induce apoptosis in tumor cells. J.Biol.Chem. 274 13451 PMID: 10224110
Titov et al (2011) XPB, a subunit of TFIIH, is a target of the natural product triptolide. Nat.Chem.Biol. 7 182 PMID: 21278739
If you know of a relevant reference for Triptolide, please let us know.
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关键词: Triptolide, Triptolide supplier, Blocks, TNF-α, TNF-alpha-mediated, c-IAP2, c-IAP1, induction, inhibitors, inhibits, apoptosis, TNF-alpha-induced, NF-κB, NF-kappaB, NF-kB, activation, X-Linked, Apoptosis, XIAP, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, Transcription, Factors, Immunosuppressants, DNA, Polymerase, RNA, DNA,, and, Protein, Synthesis, Inhibitor, of, (IAP), 3253, Tocris Bioscience
8 篇 Triptolide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Triptolide 的部分引用包括：
Shao et al (2019) Reporter-ChIP-nexus reveals strong contribution of the Drosophila initiator sequence to RNA polymerase pausing. Elife 8 PMID: 31021316
Tettey et al (2019) A Role for FACT in RNA Polymerase II Promoter-Proximal Pausing. Cell Rep 27 3770 PMID: 31242411
Vollmer et al (2012) Anti-inflammatory effects of mapracorat, a novel selective glucocorticoid receptor agonist, is partially mediated by MAP kinase phosphatase-1 (MKP-1). J Biol Chem 287 35212 PMID: 22898817
Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005
Filone et al (2014) The master regulator of the cellular stress response (HSF1) is critical for orthopoxvirus infection. PLoS Pathog 10 e1003904 PMID: 24516381
Petropoulos et al (2024) Transcription-replication conflicts underlie sensitivity to PARP inhibitors. Nature 628 433 PMID: 38509368
Liao and Mizzen (2017) Site-specific regulation of histone H1 phosphorylation in pluripotent cell differentiation. Epigenetics Chromatin 10 29 PMID: 28539972
Zhao et al (2015) Hyaluronic acid prevents immunosuppressive drug-induced ovarian damage via up-regulating PGRMC1 expression. Sci Rep 5 7647 PMID: 25558795
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Triptolide 的评论
平均评分: 5 (Based on 1 Review.)
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Works well.
By
Anonymous on 06/22/2020
分析类型： In Vitro
种属： Human
细胞系/组织： U2OS
triptolide (1 μM)
I used short treatments with the transcription inhibitors triptolide. These inhibited ongoing RNA synthesis and increased replication fork speeds specifically in the presence of JQ1
