PI3KC2α-IN-1

• 常用名: PI3KC2α-IN-1
• 英文名: PI3KC2α-IN-1
• CAS号: 2397679-87-5
• 分子量: 424.50
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₁₆N₆O₂S₂
• 熔点: N/A
• 闪点: N/A

PI3KC2α-IN-1用途

PI3KC2α-IN-1是一种有效的PI3KC3α抑制剂(IC50:95 nM)。IN-1与PI3KC2α的ATP结合位点相互作用。PI3KC2α-IN-1可用于血栓形成、糖尿病和癌症的研究[1]。

PI3KC2α-IN-1名称

• 英文名: PI3KC2α-IN-1

PI3KC2α-IN-1生物活性

• 描述: PI3KC2α-IN-1是一种有效的PI3KC3α抑制剂(IC50:95 nM)。IN-1与PI3KC2α的ATP结合位点相互作用。PI3KC2α-IN-1可用于血栓形成、糖尿病和癌症的研究[1]。
• 相关类别:
  研究领域 >> 癌症
  研究领域 >> 心血管疾病
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K
  研究领域 >> 代谢疾病
• 靶点实验:

  PI3KC2α:95 nM (IC50)

  PI3KC2β:5700 nM (IC50)

  PI3KC2γ:860 nM (IC50)

• 体外研究: PI3KC2α-IN-1(PITCOIN1,30 nM-1 mM,HEK293T细胞裂解物)在靶向PI3KC2α方面具有高度选择性,但没有其他人激酶(Kinobead分析法)[1]。PI3KC2α-IN-1(100μM,20 h)在HeLa细胞中没有检测到细胞毒性[1]。PI3KC2α-IN-1(6 h)阻断eGFP–SNX9诱导的HeLa细胞质膜微管化(EC50:5μM)[1]。PI3KC2α-IN-1(20μM,6 h)会导致Cos7细胞中网织红介导的转铁蛋白内吞受损[1]。PI3KC2α-IN-1(20μM,6 h)抑制内体PI(3)P合成[1]。PI3KC2α-IN-1(20μM,6 h)损害小鼠静息血小板的血小板膜和血栓形成[1]。细胞活力测定[1]细胞系：Cos7细胞浓度：20μM孵育时间：6小时结果：降低内体PI(3)P,并降低PI(3)P结合效应物早期内体抗原1(EEA1)的内体膜募集。

PI3KC2α-IN-1物理化学性质

• 分子式: C₁₉H₁₆N₆O₂S₂
• 分子量: 424.50
• InChIKey: ANHMCIKPOJARRV-UHFFFAOYSA-N
• SMILES: O=C(CSc1nc2nccnc2c(=O)n1CCc1ccccc1)Nc1nccs1

PI3KC2α-IN-1靶点实验

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实验名称：Selectivity ratio of IC50 for inhibition of PI3KC2beta(unknown origin) to IC50 for in... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5373586

实验名称：Inhibition of recombinant GST-tagged human PI3KC2alpha (142 to 1412 residues) express... 来源：ChEMBL 靶标：Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha External Id：CHEMBL5373587

实验名称：Inhibition of PI3KC2alpha deltaN domain (unknown origin) preincubated for 5 mins foll... 来源：ChEMBL 靶标：Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha External Id：CHEMBL5373584

实验名称：Cytotoxicity against African green monkey COS-7 cells assessed as LDH release at 100 ... 来源：ChEMBL 靶标：COS-7 External Id：CHEMBL5373592

实验名称：Inhibition of PI4Kbeta (unknown origin) at 10 uM relative to control 来源：ChEMBL 靶标：Phosphatidylinositol 4-kinase beta External Id：CHEMBL5373591

实验名称：Inhibition of PI3KC2beta (unknown origin) using PI lipid kinase as substrate in the p... 来源：ChEMBL 靶标：Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta External Id：CHEMBL5373588

实验名称：Inhibition of PI3KC2gamma (unknown origin) in the presence of 10 uM ATP by Adapta uni... 来源：ChEMBL 靶标：Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma External Id：CHEMBL5373589

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