TR-07
TR-07 is a PRMT1 activator. TR-07 binds to the αY helix near the catalytic core to enhance PRMT1 homodimerization and catalytic activity, induces apoptosis in pancreatic cancer cells, and reduces cell viability. TR-07 can be used for research on pancreatic ductal adenocarcinoma and pancreatic cancer.
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。
- 分子式: C20H21N3O2
- 分子量:335.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- プロトコル
- 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
IC50 & Target
[1]|
PRMT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PANC-1 | IC50 |
45 μM
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Cytotoxicity against human PANC-1 pancreatic tumor cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay.
Cytotoxicity against human PANC-1 pancreatic tumor cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay.
|
42720487 |
体外実験
TR-07 (1-2 h) enhances the enzymatic activity of PRMT1 toward natural and physiologically relevant substrates such as histone H2A, H4, and GAR[1].
TR-07 (100 μM), as an activator of PRMT1, increases its catalytic activity by 45% at 100 μM, while having no significant effect on PRMT6[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 pancreatic tumor cells
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Concentration:10; 20 μM
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Incubation Time:72 h
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Result:Resulted in a concentration-dependent increase in global arginine methylation compared to DMSO-treated control cells.
体内実験
TR-07 (2 weeks) treatment increases cellular ADMA levels in PANC-1 tumor xenografts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (female, 9-15 weeks, 20-30 g, subcutaneous xenograft)[1]
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Dosage:150 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly reduced tumor growth compared to the PBS control group.
Further significantly reduced tumor growth in combination with gemcitabine compared to monotherapies.
Elevated mean intensity ADMA levels in PANC-1 xenografts upon application, both as monotherapy and in combination with gemcitabine, compared to PBS or gemcitabine alone.
Exhibited no significant adverse or systemic toxic effects at the applied doses.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- CCK-8/WST-8 Cell Proliferation Assay
- MTT Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
化学情報
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分子量 335.40
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分子式 C20H21N3O2
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SMILES
CN(CC1=CC(C/N=C/C2=C(NC(C3=CC=CC=C32)=O)O)=CC=C1)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TR-07 関連分類
HY-189431 関連分類
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