受注:045-509-1970 |
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Synonyms | EPZ015866, GSK3203591 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H28N4O2 |
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分子量 | 380.48 | CAS No. | 1616391-87-7 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 76 mg/mL (199.74 mM) | ||||||||
Ethanol | 76 mg/mL (199.74 mM) | ||||||||||
Water | Insoluble | ||||||||||
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 | GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM. |
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in vitro | In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases[2][3]. |
細胞アッセイ | 細胞株 | Cell-free assays |
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濃度 | 4 nM | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | BALB/C nude mice |
投薬量 | 50 mg/kg | |
投与方法 | s.c. |
Data from [Data independently produced by , , Cancer Med, 2018, 7(3):869-882]
(S)-2-(Cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide Attenuates RANKL-Induced Osteoclast Differentiation by Inhibiting NF-κB Nuclear Translocation [ Int J Mol Sci, 2023, 24(5)4327] | PubMed: 36901758 |
Global profiling of arginine dimethylation in regulating protein phase separation by a steric effect-based chemical-enrichment method [ Proc Natl Acad Sci U S A, 2022, 119(43):e2205255119] | PubMed: 36256816 |
HBV covalently closed circular DNA minichromosomes in distinct epigenetic transcriptional states differ in their vulnerability to damage [ Hepatology, 2021, 10.1002/hep.32245] | PubMed: 34779008 |
HBV covalently closed circular DNA minichromosomes in distinct epigenetic transcriptional states differ in their vulnerability to damage [ Hepatology, 2021, 10.1002/hep.32245] | PubMed: 34779008 |
PRMT5 Inhibition Promotes PD-L1 Expression and Immuno-Resistance in Lung Cancer [ Front Immunol, 2021, 12:722188] | PubMed: 35111150 |
An AKT/PRMT5/SREBP1 axis in lung adenocarcinoma regulates de novo lipogenesis and tumor growth [ Cancer Sci, 2021, 10.1111/cas.14988] | PubMed: 34033176 |
Arginine methylation of SHANK2 by PRMT7 promotes human breast cancer metastasis through activating endosomal FAK signalling [ Elife, 2020, 9e57617] | PubMed: 32844749 |
Immunogenicity of prostate cancer is augmented by BET bromodomain inhibition. [ J Immunother Cancer, 2019, 7(1):277] | PubMed: 31653272 |
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] | PubMed: 30135193 |
PRMT 5 promotes cell proliferation by inhibiting BTG 2 expression via the ERK signaling pathway in hepatocellular carcinoma [Jiang H Cancer Med, 2018, 7(3):869-882] | PubMed: 29441724 |
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。