PIK-108

• 常用名: PIK-108
• 英文名: PIK-108
• CAS号: 901398-68-3
• 分子量: 364.44
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₂₄N₂O₃
• 熔点: N/A
• 闪点: N/A

PIK-108用途

PIK-108 是一种非 ATP 竞争性的,变构的 p110β/p110δ 选择性抑制剂。

PIK-108名称

• 英文名: PIK-108

PIK-108生物活性

• 描述: PIK-108 是一种非 ATP 竞争性的,变构的 p110β/p110δ 选择性抑制剂。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K
• 体外研究: PIK-108(0.1-10μM；1小时)阻断PKB/Akt的磷酸化[1]。Western Blot分析[1]细胞系：表达野生型PTEN的胶质瘤细胞系浓度：0.1,0.5,1,4,结果：突变体PTEN表达细胞的PKB/Akt磷酸化水平有不同程度的抑制作用,但与野生型PTEN表达细胞相比,突变型PTEN表达细胞的PKB/Akt磷酸化水平明显降低。
• 参考文献:

  [1]. Zachary A Knight, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

  [2]. Jack S Chen, et al. Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Mol Cancer Ther. 2008 Apr;7(4):841-50.

PIK-108物理化学性质

• 分子式: C₂₂H₂₄N₂O₃
• 分子量: 364.44
• InChIKey: VRCXIJAYLCUSHC-UHFFFAOYSA-N
• SMILES: Cc1cc(C(C)Nc2ccccc2)c2oc(N3CCOCC3)cc(=O)c2c1

PIK-108靶点实验

查看更多实验

实验名称：Inhibition of PI3Kdelta (unknown origin) 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform External Id：CHEMBL3223609

实验名称：Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus inf... 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform External Id：CHEMBL2067455

实验名称：Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus inf... 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform External Id：CHEMBL2067458

实验名称：Inhibition of N-terminus poly-His tagged human PI3Kbeta expressed in baculovirus infe... 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform External Id：CHEMBL2067456

实验名称：Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insec... 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform External Id：CHEMBL2067457

实验名称：Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed i... 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform External Id：CHEMBL2067908

实验名称：Selectivity ratio of IC50 for human PI3Kbeta-mediated Akt phosphorylation at T308 res... 来源：ChEMBL 靶标：N/A External Id：CHEMBL2067909

实验名称：Inhibition of PI3Kalpha (unknown origin) 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform External Id：CHEMBL3223603

实验名称：Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient... 来源：ChEMBL 靶标：N/A External Id：CHEMBL2067907

实验名称：Inhibition of PI3Kbeta (unknown origin) 来源：ChEMBL 靶标：Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform External Id：CHEMBL3223602

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