|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; BDBM195601|
SCHEMBL14831541, also called as Mutant IDH1 inhibitor, is an inhibitor of mutant IDH1 which is key enzymes found in cellular metabolism.
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Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).
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.