IC-87114
产品说明书
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同义名 : | - |
| CAS号 : | 371242-69-2 | |
| 货号 : | A937152 | |
| 分子式 : | C22H19N7O | |
| 纯度 : | 99%+ | |
| 分子量 : | 397.43 | |
| MDL号 : | MFCD09970845 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
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| 描述 | IC-87114 has been synthesized to assess its selectivity for PI3Kδ relative to other class I PI3Ks. The IC50 for PI3Kδ inhibition by IC-87114 is 0.5μM, while the IC50 values for PI3Kα, PI3Kβ, and PI3Kγ are >100μM, 75μM, and 29μM, respectively. This demonstrates that IC-87114 is 58-fold more selective for PI3Kδ compared to PI3Kγ, and exhibits over 100-fold selectivity relative to PI3Kα and PI3Kβ. IC-87114 selectively antagonizes PI3Kδ over a concentration range of 0.3-10μM[1]. IC-87114, at a concentration of 10μM, is utilized to selectively target PI3Kδ catalytic function. This concentration of IC-87114 successfully deactivates Akt in macrophages after a 1-hour treatmen. Subsequently, the impact of IC-87114 on AP-1 DNA-binding activity is assessed. The electrophoretic mobility shift assay reveals that AP-1 DNA-binding activity significantly rises following TNF-α treatment (10/20 ng/mL). IC-87114 alone prompts AP-1 DNA-binding activity post 1-hour treatment. Moreover, the combination of IC-87114 (10μM) with TNF-α (0-20 ng/mL) results in stronger AP-1 DNA-binding activity than TNF-α alone. Additionally, IC-87114 (10μM) effectively curtails p110δ catalytic activities (Akt phosphorylation) in macrophages, irrespective of TNF-α treatment over 24 hours[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.16mL 5.03mL 2.52mL |
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