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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder |
化学式 | C17H18N4O4 |
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分子量 | 342.35 | CAS No. | 2040291-27-6 | |
Solubility (25°C)* | 体外 | DMSO | 68 mg/mL (198.62 mM) | |
Water | 8 mg/mL (23.36 mM) | |||
Ethanol | 2 mg/mL (5.84 mM) | |||
* <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 | LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity. |
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in vitro | LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members.[1] |
in vivo | LLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition.[1] |
細胞アッセイ | 細胞株 | Sf9 cells, A375 tumor cells, MCF7 cells |
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濃度 | 1 µM, 10 µM | |
反応時間 | 48 h | |
実験の流れ | PRMT5 cellular assay. MCF7 cells are grown in DMEM supplemented with 10% FBS, penicillin (100 units/ml) and streptomycin (100 µg/ml). 40% confluent cells are treated with different concentrations of LLY-283 or DMSO control for 48 h. The levels of SmBB' and symmetrically dimethylated SmBB' are analyzed in westernblot. |
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動物実験 | 動物モデル | SCID mice with A375 derived xenografts |
投薬量 | 20 mg/kg | |
投与方法 | Oral gavage |
Long non-coding RNA-derived peptides are immunogenic and drive a potent anti-tumour response [ Nat Commun, 2023, 14(1):1078] | PubMed: 36841868 |
Inhibition of histone methyltransferase PRMT5 attenuates cisplatin-induced hearing loss through the PI3K/Akt-mediated mitochondrial apoptotic pathway [ J Pharm Anal, 2023, 13(6):590-602] | PubMed: 37440906 |
A PRMT5 inhibitor protects against noise-induced hearing loss by alleviating ROS accumulation [ Ecotoxicol Environ Saf, 2022, 243:113992] | PubMed: 35994911 |
Explore the effect of LLY-283 on the ototoxicity of auditory cells caused by cisplatin: A bioinformatic analysis based on RNA-seq [ J Clin Lab Anal, 2022, e24176] | PubMed: 34997776 |
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。