| Description | NCT-504, a selective allosteric inhibitor of PIP4Kγ, exhibits an IC50 value of 15.8 μM. It holds promise for the investigation of Huntington's disease. |
| In vitro | NCT-504在缺乏PI5P底物的情况下，不影响PIP4Kγ的本征ATP水解活性[1]。此外，NCT-504不抑制PIP4Kbeta，并且对PIP4Kalpha磷酸化PI5P的抑制作用较弱[1]。在50 μM的浓度下，NCT-504既不抑制PIP4Kbeta也不抑制PIP4Kalpha（IC 50在50 μM到100 μM之间）[1]。NCT-504能提高MEFs中PI(3,5)P2、PI3P和PI5P的水平[1]。在10 μM浓度、作用12小时的条件下，NCT-504对MEFs的细胞活性没有影响[1]。NCT-504（5 μM、10 μM；2小时、6小时）提高了自噬的诱导以及自噬货物周转率[1]。NCT-504处理显著增加了自溶体的形成，同时只轻微提高了自噬体的数量[1]。NCT-504增加了293A细胞中的自噬流量并减少了亨廷顿蛋白[1]。在携带亨廷顿病基因敲入鼠源的不死化纹状体细胞中，NCT-504降低了mHtt蛋白水平[1]。西方印迹分析[1]细胞系：HEK293T细胞；浓度：5 μM、10 μM；孵育时间：2小时、6小时；结果：诱导自噬体的形成。 |
| Target activity | PIP4Kγ:15.8 μM (IC50) |
| molecular weight | 404.49 |
| Molecular formula | C15H12N6O2S3 |
| CAS | 1222765-97-0 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 112.5 mg/mL (278.1 mM), Sonication is recommended. |
| References | 1. Ismael Al-Ramahi, et al. Inhibition of PIP4Kγ Ameliorates the Pathological Effects of Mutant Huntingtin Protein. Elife. 2017 Dec 26;6:e29123. |