产品
编 号:F339276
分子式:C22H19N7O
分子量:397.43
产品类型
结构图
CAS No: 371242-69-2
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产品详情
生物活性:
IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.
体内研究:
Treatment with PD 89059 (10?mg/kg), IC-87114 (0.3?mg/kg) and BAY 11-7085 (10?mg/kg), significantly (P0.05). 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.
体外研究:
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; PIC-87114 相关抗体: