NCT-504

• 常用名: NCT-504
• 英文名: NCT-504
• CAS号: 1222765-97-0
• 分子量: 404.49
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₅H₁₂N₆O₂S₃
• 熔点: N/A
• 闪点: N/A

NCT-504用途

NCT-504 是选择性的脂质激酶 PIP4Kγ 变构抑制剂,其 IC50 值为 15.8 μM。NCT-504 具有用于亨廷顿氏症疾病研究的潜力。

NCT-504名称

• 英文名: NCT-504

NCT-504生物活性

• 描述: NCT-504 是选择性的脂质激酶 PIP4Kγ 变构抑制剂,其 IC50 值为 15.8 μM。NCT-504 具有用于亨廷顿氏症疾病研究的潜力。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 靶点实验:

  IC50: 15.8 μM (PIP4Kγ)[1]

• 体外研究: NCT-504在没有PI5P底物的情况下不影响PIP4Kγ的内源性ATP水解活性[1]。NCT-504不抑制PIP4Kbeta,弱抑制PI5P的pip4kapha磷酸化[1]。NCT-504在50μM浓度下不抑制PIP4Kbeta或PIP4Kalpha(IC50在50μM和100μM之间)[1]。NCT-504提高了MEFs中PI(3,5)P2、PI3P和PI5P的水平[1]。NCT-504(10μM；12小时)对MEFs中的细胞活力没有影响[1]。NCT-504(5μM,10μM；2小时,6小时)提高了自噬诱导和自噬货物周转率[1]。NCT-504治疗可使自溶体的形成显著增加,自噬体的形成仅略有升高[1]。NCT-504增加了293A细胞的自噬通量,降低了亨廷顿蛋白[1]。NCT-504降低敲除HD小鼠永生化纹状体细胞mht蛋白水平[1]。Western Blot分析[1]细胞系：HEK293T细胞浓度：5μM,孵育时间：2小时,6小时结果：诱导自噬体形成。
• 参考文献:

  [1]. Ismael Al-Ramahi, et al. Inhibition of PIP4Kγ Ameliorates the Pathological Effects of Mutant Huntingtin Protein. Elife. 2017 Dec 26;6:e29123.

NCT-504物理化学性质

• 分子式: C₁₅H₁₂N₆O₂S₃
• 分子量: 404.49
• InChIKey: IIEFAIOSYLQBJX-UHFFFAOYSA-N
• SMILES: Cn1nnnc1Sc1ncnc2scc(-c3cccc(S(C)(=O)=O)c3)c12

NCT-504靶点实验

查看更多实验

实验名称：NCATS Kinetic Aqueous Solubility Profiling 来源：NCGC 靶标：N/A External Id：ADME-solubility1

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling 来源：NCGC 靶标：N/A External Id：ADME-PAMPA1

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Primary qHTS for Identification of Calcium Integrin Binding Protein 1 (CIB1) Competit... 来源：NCGC External Id：CIB1-p1-p2

共120条，当前第1页，共12页

1

2

3

4

5