LLY-283

製品コードS8883 バッチS888301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C17H18N4O4
分子量 342.35 CAS No. 2040291-27-6
Solubility (25°C)* 体外 DMSO 68 mg/mL (198.62 mM)
Water 5 mg/mL (14.6 mM)
Ethanol 3 mg/mL (8.76 mM)
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.4mg/ml Taking the 1 mL working solution as an example, add 50 μL 68 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Sf9 cells, A375 tumor cells, MCF7 cells
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.
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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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