| Identification | Back Directory | [Name]
Thieno[2,3-d]pyrimidine, 5-[3-(methylsulfonyl)phenyl]-4-[(1-methyl-1H-tetrazol-5-yl)thio]- | [CAS]
1222765-97-0 | [Synonyms]
NCT-504
Thieno[2,3-d]pyrimidine, 5-[3-(methylsulfonyl)phenyl]-4-[(1-methyl-1H-tetrazol-5-yl)thio]- | [Molecular Formula]
C15H12N6O2S3 | [MDL Number]
MFCD34470420 | [MOL File]
1222765-97-0.mol | [Molecular Weight]
404.49 |
| Chemical Properties | Back Directory | [Boiling point ]
740.3±70.0 °C(Predicted) | [density ]
1.67±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (309.03 mM; Need ultrasonic) | [form ]
Solid | [pka]
0.22±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease[1]. | [Definition]
ChEBI: 5-(3-methylsulfonylphenyl)-4-[(1-methyl-5-tetrazolyl)thio]thieno[2,3-d]pyrimidine is an aryl sulfide and a thienopyrimidine. | [Biological Activity]
NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease[1].
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 (IC50 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]. | [References]
[1]. Ismael Al-Ramahi, et al. Inhibition of PIP4Kγ Ameliorates the Pathological Effects of Mutant Huntingtin Protein. Elife. 2017 Dec 26;6:e29123. |
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