| Identification | Back Directory | [Name]
GSK864 | [CAS]
1816331-66-4 | [Synonyms]
GSK864
GSK864 >=98% (HPLC)
1H-Pyrazolo[4,3-c]pyridine-3,7-dicarboxamide, 1-[(4-fluorophenyl)methyl]-4,5,6,7-tetrahydro-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-, (7S)- | [Molecular Formula]
C30H31FN6O4 | [MDL Number]
MFCD30478507 | [MOL File]
1816331-66-4.mol | [Molecular Weight]
558.6 |
| Chemical Properties | Back Directory | [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) | [form ]
powder | [pka]
11.73±0.70(Predicted) | [color ]
white to beige | [optical activity]
[α]/D -66 to -76°, c = 0.5 in methanol |
| Hazard Information | Back Directory | [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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