Tanshindiol C
Based on 1 Customer Validation
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.47%
- CAS 番号: 97465-71-9
- 分子式: C18H16O5
- 分子量:312.32
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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EZH2 0.55 μM (IC50) |
SIRT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
4.2 μM
Compound: 5
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Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
| Daudi | GI50 |
10.6 μM
Compound: 5
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Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
| PC-3 | GI50 |
4 μM
Compound: 5
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Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
| Pfeiffer | GI50 |
1.5 μM
Compound: 5
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Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
| T98G | GI50 |
6 μM
Compound: 5
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Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
| U2932 | GI50 |
9.5 μM
Compound: 5
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Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
| U-87MG ATCC | GI50 |
5.7 μM
Compound: 5
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Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay
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[PMID: 24767850] |
体外実験
Tanshindiol C (1-10 μM; for 24 h) activates Nrf2 and upregulates Prdx1 expression and mRNA levels in macrophages. Tanshindiol C protects macrophages from oxidized low-density lipoprotein (oxLDL) induced foam cell formation via activation of Prdx1/ABCA1 signaling[1].
Tanshindiol C inhibits both wild-type and A667G mutant (Ki value of 176 nM) EZH2 activity with similar potencies[2].
Tanshindiol C inhibits growth of the cell lines such as Pfeiffer, U-2932 and Daudi (lymphoma), PC3 (prostate cancer), T98G and U87MG (glioma), and A549 (lung cancer), with GI50 values of 1.5 μM, 9.5 μM, 10.6 μM, 4 μM, 6 μM, 5.7 μM and 4.2 μM, respectively[2].
Tanshindiol C (1-5 μM; 72 hours) induces accumulation of Pfeiffer cells in sub-G1 phase, which indicates cells in late apoptosis and necrosis[2].
Tanshindiol C (1-3 μM; 72 hours) increases protein levels of the important apoptosis related protein markers, cleaved caspase-3, caspase-7 and poly ADP-ribose polymerase (PRAP) in the cells.Tanshindiol C significantly decreases the levels of H3K27me3 in cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Upregulated the Nrf2 and Prdx1 mRNA levels.
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Cell Line:Mouse peritoneal macrophages
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Concentration:1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Activated Nrf2 and upregulated Prdx1 expression in macrophages.
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Cell Line:Pfeiffer cells
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Concentration:1 μM, 2.5 μM and 5 μM
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Incubation Time:72 hours
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Result:Induced accumulation of Pfeiffer cells in sub-G1 phase.
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Cell Line:Pfeiffer cells
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Concentration:1 μM, 3 μM
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Incubation Time:72 hours
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Result:The levels of H3K27me3 was significantly decreased in the cells.
化学情報
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CAS 番号 97465-71-9
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性状 Solid
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分子量 312.32
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分子式 C18H16O5
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Color Brown to red
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SMILES
O=C(C1=C2C=CC3=C1CC[C@@H](O)[C@@]3(O)C)C(C4=C2OC=C4C)=O
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (80.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Yuyu Yang, et al. Tanshindiol C inhibits oxidized low-density lipoprotein induced macrophage foam cell formation via a peroxiredoxin 1 dependent pathway. Biochim Biophys Acta Mol Basis Dis. 2018 Mar;1864(3):882-890. [Content Brief]
[2]. Jimin Woo, et al. Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2486-92. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | 80.0461 mL |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | 16.0092 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 mL | 8.0046 mL | |
| 15 mM | 0.2135 mL | 1.0673 mL | 2.1346 mL | 5.3364 mL | |
| 20 mM | 0.1601 mL | 0.8005 mL | 1.6009 mL | 4.0023 mL | |
| 25 mM | 0.1281 mL | 0.6404 mL | 1.2807 mL | 3.2018 mL | |
| 30 mM | 0.1067 mL | 0.5336 mL | 1.0673 mL | 2.6682 mL | |
| 40 mM | 0.0800 mL | 0.4002 mL | 0.8005 mL | 2.0012 mL | |
| 50 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3341 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0006 mL |
Tanshindiol C 関連分類
HY-122936 関連分類
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