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IC-87114

CAS No. : 371242-69-2

MCE 国际站：IC-87114

产品活性：IC-87114 是一种有效的选择性 PI3Kδ 抑制剂，IC₅₀ 为 0.5 µM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: IC-87114 (IC87114), an analog of the original inhibitor, is synthesized and tested for PI3Kδ selectivity relative to the other class I PI3Ks. The IC₅₀ of IC87114 for PI3Kδ inhibition is 0.5 µM whereas the IC₅₀ values for PI3Kα, PI3Kβ, and PI3Kγ are >100, 75, and 29 µM, respectively. Thus IC87114 is 58-fold more selective for PI3Kδ relative to PI3Kγ, and over 100-fold selective relative to PI3Kα and PI3Kβ. IC87114 selectively antagonizes PI3Kδ over at least a concentration range of 0.3-10 µM. IC-87114 (10 µM) is also used to selectively inhibit PI3Kδ catalytic activity to address this question. IC87114 (10 µM) 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-α (10 ng/mL; P<0.001) and TNF-α (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 µM) and TNF-α (0-20 ng/mL) than only treatment with TNF-α (0-20 ng/mL; n=5; P<0.01). IC87114 (10 µM) also effectively inhibits p110δ catalytic activities (Akt phosphorylation) in macrophages with or without TNF-α treatment for 24 hours (n=6; P<0.001).

In Vivo: Treatment with PD 89059 (10 mg/kg), IC-87114 (0.3 mg/kg) and BAY 11⁻⁷085 (10 mg/kg), significantly (P<0.05) reduces the OVA- induced inflammatory cell influx into the airways and the histopathological airway remodeling. However, these treatments does not significantly improve OVA induced-AHR (P>0.05). Of note, the observed reduction in the histopathological airway remodeling induced by PD 89059, IC-87114 and BAY 11⁻⁷085 are less effective as compared to the reduction seen with AG 1478 and SU6656.

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