產(chǎn)品目錄

規(guī)格	10mg 50mg 500mg 1g
CAS	1793053-37-8
別名	N/A
化學名	5-cyano-2'-(4-(2-(3-methyl-1H-indol-1-yl)ethyl)piperazin-1-yl)-N-(3-(pyrrolidin-1-yl)propyl)-[1,1'-biphenyl]-3-carboxamide
分子式	C36H42N6O
分子量	574.76
溶解度	≥ 57.5mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

IC50: < 15 nM

LLY-507 is a potent inhibitor of SMYD2.

SMYD2, a lysine methyltransferase, catalyzes the monomethylation of several protein substrates including p53. SMYD2 is reported to be overexpressed in a significant percentage of esophageal squamous primary carcinomas, and such overexpression related with poor patient survival.

In vitro: LLY-507 has been identified as a cell-active, potent small molecule inhibitor of SMYD2. LLY-507 was found to be >100-fold selective for SMYD2 over a broad range of methyltransferase and non-methyltransferase targets. The crystal structure of SMYD2 in complex with LLY-507 showed it bound in the substrate peptide binding pocket. LLY-507 was active in cells as demonstrated by the reduction of SMYD2-induced monomethylation of p53 Lys(370) at submicromolar concentrations. Furthermore, MS-based proteomics indicated that cellular histone methylation levels were not affected by SMYD2 inhibition with LLY-507 significantly, and subcellular fractionation studies showed that SMYD2 was primarily cytoplasmic, indicating that SMYD2 targeted a small subset of histones. Moreover, LLY-507 was able to inhibit the proliferation of several liver, esophageal, as well as breast cancer cell lines in a dose-dependent manner [1].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術有限公司

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