IC-87114

Short Summary : PI3Kδ inhibitor

Category : PI3K/Akt/mTOR Signaling|PI3K

Purity : 0.98

CAS Number : 371242-69-2

Formula : C22H19N7O

Molecular Weight : 397.43

SMILE : CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C=NC5=C4N=CN=C5N

Solubility : Limited solubility

Storage : Store at -20°C

Description : IC87114 is a PI(3)K selective inhibitor with IC50 of 50 nM.It has been reported that IC87114 reduced FMLP-induced PIP3 synthesis and chemotaxis in neutrophils[1]. IC87114 also blocked TNF1-stimulated elastase exocytosis from neutrophils in a mouse model of inflammation. A role for PI3K in TNF-induced signaling was demonstrated by a reduction in Akt-phosphorylation and PDK1 enzyme activity upon treatment of this cell type with IC87114 [2]. In human memory T cells, IC87114 largely inhibited T-cell receptor-induced PI(3)K signaling by both naive and effector. Cytokine production in memory T cells was blocked by IC87114 from healthy and allergic donors, or from inflammatory arthritis patients [3]. References:[1]. Workman P, van Montfort RL. PI(3) kinases: revealing the delta lady. Nat Chem Biol. 2010 Feb;6(2):82-3.[2]. Puri KD, Doggett TA, Douangpanya J, Hou Y, Tino WT, Wilson T, Graf T, Clayton E, Turner M, Hayflick JS, Diacovo TG. Mechanisms and implications of phosphoinositide 3-kinase delta in promoting neutrophil trafficking into inflamed tissue. Blood. 2004 May 1;103(9):3448-56. [3]. Soond DR, Bj rgo E, Moltu K, Dale VQ, Patton DT, Torgersen KM, Galleway F, Twomey B, Clark J, Gaston JS, Taskn K, Bunyard P, Okkenhaug K. PI3K p110delta regulates T-cell cytokine production during primary and secondary immune responses in mice and humans. Blood. 2010 Mar 18;115(11):2203-13.

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