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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
| Molecular Weight | 558.6 |
| Formula | C30H31FN6O4 |
| CAS Number | 1816331-66-4 |
| Form | Solid |
| Solubility (25°C) | DMSO: 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Isocitrate Dehydrogenase (IDH) Products |
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| Enasidenib
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively. |
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| Ivosidenib
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