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Synonyms | EPZ019997 3HCl | Storage (From the date of receipt) |
3 years -20°C powder | ||||||||
化学式 | C20H41Cl3N4O2 |
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分子量 | 475.92 | CAS No. | 2227587-26-8 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 81 mg/mL (170.19 mM) | ||||||||
Water | 81 mg/mL (170.19 mM) | ||||||||||
Ethanol | 81 mg/mL (170.19 mM) | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | GSK3368715 3HCl is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM. |
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in vitro | GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.[1] |
in vivo | GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.[1] |
細胞アッセイ | 細胞株 | 249 cancer cell lines (Toledo cells, BxPC3 cells, MiaPaca-2 cells, ACHN cells, MDA-MB-468 cells, RKO cells, Panc03.27 cells, etc.) |
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濃度 | 0.75 nM, 2 μM | |
反応時間 | 30 min, 3 h - 168 h | |
実験の流れ | In Cell Western. RKO cells are seeded in a clear bottom 384 well plates andtreated with a 20-point two-fold dilution series of GSK3368715 (29,325.5 to 0.03 nM) or 0.15% DMSO. Plates are incubated for 3 days at 37℃ in 5% CO2. Cells are fixed with ice-cold methanol for 30 minutes at room temperature, washed with phosphate buffered saline (PBS), then incubated with Odyssey blocking buffer (Licor) for 1 hour at room temperature. | |
動物実験 | 動物モデル | Female NMRI nu/nu mice (NMRI-Foxn1nu) implanted with tumor fragment |
投薬量 | 75 mg/kg, 150 mg/kg, 300 mg/kg | |
投与方法 | Oral gavage |
PRMT1 mediated methylation of cGAS suppresses anti-tumor immunity [ Nat Commun, 2023, 14(1):2806] | PubMed: 37193698 |
FACS-based genome-wide CRISPR screens define key regulators of DNA damage signaling pathways [ Mol Cell, 2023, 83(15):2810-2828.e6] | PubMed: 37541219 |
Epigenetic drug screening defines a PRMT5 inhibitor-sensitive pancreatic cancer subtype [ JCI Insight, 2022, 7(10)e151353] | PubMed: 35439169 |
Modulation of IKs channel-PIP2 interaction by PRMT1 plays a critical role in the control of cardiac repolarization [ J Cell Physiol, 2022, 10.1002/jcp.30775] | PubMed: 35580065 |
Purification and Identification of Natural Inhibitors of Protein Arginine Methyltransferases from Plants [ Mol Cell Biol, 2022, e0052321] | PubMed: 35311588 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。