PI3K Synthesis Inhibitor IC-87114 Cas 371242-69-2

IC-87114 (IC87114), an analog of the original inhibitor, is synthesized and tested for PI3K selectivity relative to the other class I PI3Ks. The IC₅₀of IC87114 for PI3K inhibition is 0.5 M whereas the IC₅₀values for PI3K, PI3K, and PI3K are >100, 75, and 29 M, respectively. Thus IC87114 is 58-fold more selective for PI3K relative to PI3K, and over 100-fold selective relative to PI3K and PI3K. IC87114 selectively antagonizes PI3K over at least a concentration range of 0.3-10 M. IC-87114 (10 M) is also used to selectively inhibit PI3K catalytic activity to address this question. IC87114 (10 M) effectively inactivates Akt in macrophages after treatment for 1 hour (n=6; P<0.001 versus control). The effect of IC-87114 (IC87114) is next detected ton AP-1 DNA-binding activity. The electrophoretic mobility shift assay assay demonstrates that DNA-binding activity of AP-1 is significantly increased after the treatment with TNF- (10 ng/mL; P<0.001) and TNF- (20 ng/mL; P<0.001). IC87114 alone induces AP-1 DNA-binding activity after treatment for 1 hour. Furthermore, there is stronger AP-1 DNA-binding activity after costimulation of IC87114 (10 M) and TNF- (0-20 ng/mL) than only treatment with TNF- (0-20 ng/mL; n=5; P<0.01). IC87114 (10 M) also effectively inhibits p110 catalytic activities (Akt phosphorylation) in macrophages with or without TNF- treatment for 24 hours (n=6; P<0.001).

Related Products:

Idelalisib; Almorexant HCL; Pictilisib; Pictilisib mesylate; XL147; PIK-90; Omipalisib; Buparlisib; TG100-115; A66;