现货,TGX-221 ,CAS号:663619-89-4,美国进口, PI3K / mTOR / AKT , PI3K , PI3K 抑制剂和化合物,selleck,S1169

信号转导通路: PI3K / mTOR / AKT >> PI3K >> PI3K 抑制剂和化合物 >> TGX-221http://www.dxy.cn/redirect?url=http://selleck.cn/tgx-221-S1169.html

技术数据:

分子量(MW): 364.44

化学式:

C21H24N4O2

 

溶解度: DMSO ≥17mg/mL Water <1mg/mL Ethanol ≥4mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 663619-89-4

生物活性

 

 

TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .[1,2] Thrombogenix compound TGX-221 is a LY294002 analogue, able to inhibit selectively the PI3Kβ isoform in vitro. The chromone core of LY294002 was replaced with pyrido[1,2-a] pyrimidin-4-one and inserted into an aryl ring moiety, increasing the potency and selectivity against PI3Kβ(IC50=10nM).[1]

TGX-221 is a low-nanomolar range inhibitor, shows about 1000-fold higher selectivity over PI3Kα, and is cell permeable. TGX-221 interfered with shear stress-induced PtdIns(3,4)P2 production and integrin αIIbβ3-mediated adhesion in platelets, suggesting that inhibition of PI3Kβ might have an anti-thrombotic potential in vivo.[1]

 

 

 

参考文献

Targeting phosphoinositide 3-kinase—Moving towards therapy Romina Marone,Vladimir Cmiljanovic,et al. Biochimica et Biophysica Acta 2008;1784 :159–185

PI 3-kinase p110β: a new target for antithrombotic therapy Shaun P Jackson,Simone M Schoenwaelder,et al. NATURE MEDICINE MAY 2005 ;11:507-514

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