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抑制剂 > p13k/Akt/mTOR 信号传导 > PIK-294
产品名称:
PIK-294
型号:
CS-01Y71127
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

10mM (in 1mL DMSO) 5mg 10mg 50mg 200mg

CAS

900185-02-6

别名

 

化学名

2-[[4-amino-3-(3-hydroxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one

分子式

C28H23N7O2

分子量

489.53

溶解度

24.5mg/mL in DMSO

储存条件

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

 

产品描述:                                                                                                            

IC50: 10 nM

PIK-294 is a highly selective p110δ inhibitor, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively.

Phosphoinositide 3-kinases (PI3-Ks) are a key emerging class of drug targets, but the unique roles of PI3-K isoforms remain rarely defined. Their target selectivity was biochemically enumerated that revealed cryptic homologies across targets and chemotypes by synthesizing chemically diverse panel of PI3-K inhibitors. Crystal structures of three inhibitors to p110g identify a conformationally mobile region that is uniquely exploited by bound selective compounds. This chemical array was then used to define the PI3-K isoforms required for insulin signaling.

In vitro: PIK-294 displays distinct patterns of isoform selectivity to inhibit different subsets of class I PI3K isoforms (p110β, p110δ, and p110γ) and shows low sensitivity to p110α with IC50 of 10 μM). The m-phenol moiety of PIK-294 can penetrate the deep-affinity pocket of the ATP binding site, and thus promotes in vitro inhibitory activity. PIK-294 showed one of the most potent p110d-selective inhibitors reported at present.

In vivo: PIK-294 bound p110a inhibits the acute effects of insulin treatment in vivo, whereas a p110b inhibitor has no effect.

Clinical trial: So far, no clinical study has been conducted.

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:PIK-294 

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