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。
产品描述
NCT-504 is a selective allosteric inhibitor of PIP4Kγ , with an IC 50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
体外活性
NCT-504 dose not impair the intrinsic ATP-hydrolytic activity of PIP4Kγ in the absence of PI5P substrate [1] . NCT-504 does not inhibit PIP4Kbeta and weakly inhibits PIP4Kalpha phosphorylation of PI5P [1] . NCT-504 dose not inhibit PIP4Kbeta or PIP4Kalpha (IC 50 between 50 μM and 100 μM) at 50 μM concentration [1] . NCT-504 elevates the levels of PI(3,5)P2, PI3P and PI5P in MEFs [1] . NCT-504 (10 μM; 12 hours) does not affect cell viability in MEFs [1] . NCT-504 (5 μM, 10 μM; 2 hours, 6 hours) elevates both the induction of autophagy as well as the rate of turnover of autophagic cargo [1] . NCT-504 treatment causes a robust increase in the formation of autolysosomes with only a modest elevation in autophagosomes [1] . NCT-504 increases autophagy flux and decreases huntingtin protein in 293A cells [1] . NCT-504 reduces mHtt protein levels in immortalized striatal cells from knock-in HD mice [1] . Western Blot Analysis [1] Cell Line: HEK293T cells Concentration: 5 μM, 10 μM Incubation Time: 2 hours, 6 hours Result: Induced autophagosome formation.
Cas No.
1222765-97-0
分子式
C15H12N6O2S3
分子量
404.49
别名
NCT-504
储存和溶解度
DMSO:112.5mg/mL (278.1mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years