受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H25N3O |
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分子量 | 287.40 | CAS No. | 1831110-54-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 57 mg/mL (198.32 mM) | ||||||||
Ethanol | 57 mg/mL (198.32 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 | MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively. |
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in vitro | MS023 potently reduces cellular levels of H4R3me2a in MCF7 and HEK293 cells by inhibiting PRMT1/6 methyltransferase activity with IC50 of 9 nM and 56 nM, respectively. MS023 also inhibits cell growth and potentially induces growth arrest and flattening morphology at low concentrations. MS023 displayed high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but was completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreased cellular levels of histone arginine asymmetric dimethylation. It also reduced global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells[1]. |
in vivo | MS023 is a potent, selective, and cell-active Type I PRMT inhibitor. |
キナーゼアッセイ | PRMT Biochemical Assays | |
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A scintillation proximity assay (SPA) is used for assessing the effect of test compounds on inhibiting the methyl transfer reaction catalyzed by PRMTs. In brief, the tritiated S-adenosyl-L-methionine (3H-SAM) is used as the donor of methyl group. The (3H) methylated biotin labeled peptide is captured in a streptavidin/scintillant-coated microplate, which brings the incorporated 3H-methyl and the scintillant to close proximity resulting in light emission that is quantified by tracing the radioactivity signal (counts per minute) as measured by a TopCount NXT Microplate Scintillation and Luminescence Counter. When necessary, nontritiated SAM is used to supplement the reactions. The IC50 values are determined under balanced conditions at Km concentrations of both substrate and cofactor by titration of test compounds in the reaction mixture. | ||
細胞アッセイ | 細胞株 | MCF7, U2Os, HFF, HCT116, HEK293 , A549, MDA-MB-231 and T98G |
濃度 | ~100 μM | |
反応時間 | -- | |
実験の流れ | Different cell lines are seeded on 96-well plates at density 3000/well and treated with MS023 at 0, 0.1, 1, 10, 50 and 100 μM concentrations for 96 h. MCF7, U2Os, HFF, HCT116, HEK293 are grown in DMEM and A549, MDA-MB-231 and T98G in RPMI supplemented with 10% FBS, penicillin (100 U/mL) and streptomycin (100 mg/mL). The inhibitor is replaced after 48 h. The confluency is measured using IncuCyte™ ZOOM live cell imaging device and analysed with IncuCyte™ ZOOM (2015A) software based on phase contrast images. |
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動物実験 | 動物モデル | Nude mice |
投薬量 | 80 mg/kg | |
投与方法 | i.p. |
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Inhibition of epigenetic and cell cycle-related targets in glioblastoma cell lines reveals that onametostat reduces proliferation and viability in both normoxic and hypoxic conditions [ Sci Rep, 2024, 14(1):4303] | PubMed: 38383756 |
Attenuation of protein arginine dimethylation via S-nitrosylation of protein arginine methyltransferase 1 [ Journal of Pharmacological Sciences, 2024, Pages 209-217] | PubMed: none |
PRMT1 mediated methylation of cGAS suppresses anti-tumor immunity [ Nat Commun, 2023, 14(1):2806] | PubMed: 37193698 |
PRMT blockade induces defective DNA replication stress response and synergizes with PARP inhibition [ Cell Rep Med, 2023, 4(12):101326] | PubMed: 38118413 |
PRMT1 methylates METTL14 to modulate its oncogenic function [ Neoplasia, 2023, 42:100912] | PubMed: 37269817 |
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 |
Modulating environmental signals to reveal mechanisms and vulnerabilities of cancer persisters [ Sci Adv, 2022, 8(4):eabi7711] | PubMed: 35089788 |
PRMT1 enhances oncogenic arginine methylation of NONO in colorectal cancer [ Oncogene, 2021, 40(7):1375-1389] | PubMed: 33420374 |
PRMT1 enhances oncogenic arginine methylation of NONO in colorectal cancer [ Oncogene, 2021, 10.1038/s41388-020-01617-0] | PubMed: 33420374 |
Proteome-wide Identification of Arginine Methylation in Colorectal Cancer Tissues From Patients [ Proteome Sci, 2020, 19;18:6] | PubMed: 32467672 |
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。