GSK864 Chemical Properties

Boiling point:

782.9±60.0 °C(Predicted)

Density 

1.37±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMF:20.0(Max Conc. mg/mL);35.8(Max Conc. mM)
DMSO:60.0(Max Conc. mg/mL);107.41(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);35.8(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.9(Max Conc. mM)

pka

11.73±0.70(Predicted)

form 

powder

color 

white to beige

optical activity

[α]/D -66 to -76°, c = 0.5 in methanol

GSK864 Usage And Synthesis

Biochem/physiol Actions

GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. It appears that GSK864 binds to an allosteric binding site and locks WT and mutant IDH1s in a catalytically inactive conformation. GSK864 is a highly bioavailable analog of GSK321. For full characterization details, please visit the GSK864 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc

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