Uses
TG100-115 is a potent and selective phosphoinositide 3-kinase gamma/delta (PI3Kγ/δ) inhibitor. It can provide potent cardioprotection, reduce infarct development, and preserve myocardial function.
Biological Activity
tg100-115 is an inhibitor of pi3kγ and pi3kδ with ic50 values of 83 nm and 235 nm, respectively. tg100-115 shows no obvious activity against pi3kα and pi3kβ [1].tg100-115 remarkably reduced eosinophil accumulation, balf levels of classic th2 cytokine il-13, perivascular and peribronchial leukocyte accumulations, and bronchiolar mucin accumulation in a murine model. besides, tg100-115 showed to reduce airway hyper-responsiveness (ahr) by approximately 50% in asthmatic mice. moreover, tg100-115 has been reported to reduce both smoke-and lps-induced neutrophil and lps-induced classic th1 cytokine tnfα accumulations in mice [2].
References
[1] doukas j1, wrasidlo w, noronha g, dneprovskaia e, fine r, weis s, hood j, demaria a, soll r, cheresh d. hosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. proc natl acad sci u s a. 2006 dec 26;103(52):19866-71.
[2] doukas j1, eide l, stebbins k, racanelli-layton a, dellamary l, martin m, dneprovskaia e, noronha g, soll r, wrasidlo w, acevedo lm, cheresh da. aerosolized phosphoinositide 3-kinase gamma/delta inhibitor tg100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. j pharmacol exp ther. 2009 mar;328(3):758-65.
