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LLY-284

目录号 : GC25580

LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283.

LLY-284 Chemical Structure

Cas No.:2226515-75-7

规格 价格 库存 购买数量
5mg
¥728.00
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25mg
¥2,236.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

LLY-284 is the diastereomer of LLY-283, which is a potent and selective SAM-competitive chemical probe for PRMT5. LLY-284 is much less active than LLY-283 and can be used as a negative control for LLY-283.

Chemical Properties

Cas No. 2226515-75-7 SDF Download SDF
分子式 C17H18N4O4 分子量 342.35
溶解度 DMSO: 68 mg/mL (198.63 mM);Water: Insoluble;Ethanol: 68 mg/mL (198.63 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.921 mL 14.6049 mL 29.2099 mL
5 mM 0.5842 mL 2.921 mL 5.842 mL
10 mM 0.2921 mL 1.4605 mL 2.921 mL
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Research Update

LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity

ACS Med Chem Lett 2018 Apr 23;9(7):612-617.PMID:30034588DOI:PMC6047023

Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that catalyzes the formation of symmetric dimethylarginine in a number of nuclear and cytoplasmic proteins. Although the cellular functions of PRMT5 have not been fully unraveled, it has been implicated in a number of cellular processes like RNA processing, signal transduction, and transcriptional regulation. PRMT5 is ubiquitously expressed in most tissues and its expression has been shown to be elevated in several cancers including breast cancer, gastric cancer, glioblastoma, and lymphoma. Here, we describe the identification and characterization of a novel and selective PRMT5 inhibitor with potent in vitro and in vivo activity. Compound 1 (also called LLY-283) inhibited PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively, while its diastereomer, compound 2 (also called LLY-284), was much less active. Compound 1 also showed antitumor activity in mouse xenografts when dosed orally and can serve as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells.