|Targets||Isocitrate Dehydrogenase (IDH)|
|Description||GSK321 is a highly potent, selective inhibitor of mutant IDH1 enzymes, with IC50= 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G. GSK321 stably decreased 2-hydroxyglutarate (2-HG) production in several different IDH1 mutant AML cells within a 2–3 week time frame ex vivo. Because of the allosteric nature of the interaction, GSK321 is able to inhibit multiple mutant forms of IDH1, which is consistent with our cell biological observations. Furthermore, GSK321 retains excellent potency in cells, since it does not compete with the tightly bound cofactor.|
|Appearance||Light yellow to yellow Solid|
|Synonyms||(7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; GSK321; GSK 321; GSK-321; BDBM195601|
Mutant IDH1-IN-2, aslo called as SCHEMBL14831158, is an inhibitor of mutant IDH protein. It is developed for the treatment of diseases associated with such muta...
AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
GSK864 is a cell penetrant, selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant with IC50 values of 8.8, 15.2 and 16.6 nM for IDH1 mutant...
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Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes indicated for the treatment of adult patients ...
GSK321 is a highly potent, selective inhibitor of mutant IDH1 enzymes, with IC50= 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G. GSK321 st...
AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
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