Isocitrate Dehydrogenase (IDH)
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Isocitrate dehydrogenase (IDH) is an enzyme that catalyzes the oxidative decarboxylation of isocitrate, producingalpha-ketoglutarate (α-ketoglutarate) and CO2. This is a two-step process, which involves oxidation of isocitrate (a secondary alcohol) to oxalosuccinate(a ketone), followed by the decarboxylation of the carboxyl group beta to the ketone, forming alpha-ketoglutarate. In humans, IDH exists in three isoforms: IDH3 catalyzes the third step of the citric acid cycle while converting NAD+ to NADH in the mitochondria. The isoforms IDH1 and IDH2 catalyze the same reaction outside the context of the citric acid cycle and use NADP+ as a cofactor instead of NAD+. They localize to the cytosol as well as themitochondrion and peroxisome.
Products Related to Isocitrate Dehydrogenase (IDH)(31)
- GC13147AG-221 (Enasidenib)CAS: 1446502-11-9Purity: >99.50%
AG-221 (Enasidenib) is an orally available, selective, and potent inhibitor of the mutant IDH2 enzyme, with an IC 50 value of 0.1μM and 0.4μM for IDH2 R140Q homodimer and IDH2 R172K homodimer, respectively.
- GC19059BAY-1436032CAS: 1803274-65-8Purity: >99.00%
BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
- GC19380VorasidenibCAS: 1644545-52-7Purity: >99.50%
Vorasidenib is a pan isocitrate dehydrogenase (IDH) inhibitor.
- GC31874Olutasidenib (FT-2102)CAS: 1887014-12-1Purity: >99.00%
Olutasidenib (FT-2102) (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively .
- GC32904Enasidenib mesylate (AG-221 mesylate)CAS: 1650550-25-6Purity: >99.50%
Enasidenib mesylate (AG-221 mesylate) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
- GC32966Mutant IDH1-IN-2CAS: 1429176-69-1Purity: >98.50%
Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
- GC33318Mutant IDH1-IN-4CAS: 1416270-18-2Purity: >99.00%
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
- GC34557DIM-C-pPhCO2MeCAS: 151358-48-4Purity: >99.50%
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist, with a K i value of 0.25μM.
- GC36292IDH1 Inhibitor 2CAS: 2244895-42-7Purity: >98%
IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
- GC36293IDH1 Inhibitor 3CAS: 2171081-24-4Purity: >98%
IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H.
- GC36665Mutant IDH1 inhibitorCAS: 1429180-08-4Purity: >98.50%
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
- GC38640IDH889CAS: 1429179-07-6Purity: >98.50%
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
- GC64359(R,R)-GSK321CAS: 1816272-19-1Purity: >99.00%
(R,R)-GSK321 is a mutant R132H IDH1 inhibitor with an IC 50 value of 120nM.
- GC65554IDH1 Inhibitor 1CAS: 2234285-81-3Purity: >99.00%
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity.
- GC65883(S,R)-WT IDH1 Inhibitor 2CAS: 1816272-18-0Purity: >98.00%
(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC10485 | Mutant IDH1-IN-1 | 1355326-21-4 | >99.50% | |
mutant IDH1 R132H inhibitor | ||||
| GC10531 | AGI-5198 | 1355326-35-0 | >98.00% | |
A potent, selective inhibitor of IDH1 mutations | ||||
| GC13147 | AG-221 (Enasidenib) | 1446502-11-9 | >99.50% | |
AG-221 (Enasidenib) is an orally available, selective, and potent inhibitor of the mutant IDH2 enzyme, with an IC 50 value of 0.1μM and 0.4μM for IDH2 R140Q homodimer and IDH2 R172K homodimer, respectively. | ||||
| GC14757 | AGI-6780 | 1432660-47-3 | >98.00% | |
AGI-6780 is an orally active, potent and selective mutant isocitrate dehydrogenase 2 (IDH2 R140Q ) inhibitor (IC₅₀=23±1.7nM). | ||||
| GC15601 | AG-120 | 1448347-49-6 | >98.00% | |
AG-120 (Ivosidenib) is an inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1). | ||||
| GC17809 | GSK864 | 1816331-66-4 | >98.00% | |
GSK864 is a mutant isocitrate dehydrogenases 1 (mIDH1) inhibitor, with EC 50 values of 0.16μM, 0.10μM, 2.74μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. | ||||
| GC18423 | IDH305 | 1628805-46-8 | >98.00% | |
IDH305 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively). | ||||
| GC19059 | BAY-1436032 | 1803274-65-8 | >99.00% | |
BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor. | ||||
| GC19380 | Vorasidenib | 1644545-52-7 | >99.50% | |
Vorasidenib is a pan isocitrate dehydrogenase (IDH) inhibitor. | ||||
| GC31874 | Olutasidenib (FT-2102) | 1887014-12-1 | >99.00% | |
Olutasidenib (FT-2102) (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . | ||||
| GC32904 | Enasidenib mesylate (AG-221 mesylate) | 1650550-25-6 | >99.50% | |
Enasidenib mesylate (AG-221 mesylate) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes. | ||||
| GC32966 | Mutant IDH1-IN-2 | 1429176-69-1 | >98.50% | |
Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay. | ||||
| GC33318 | Mutant IDH1-IN-4 | 1416270-18-2 | >99.00% | |
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells. | ||||
| GC34417 | (R,S)-Ivosidenib ((R,S)-AG-120) | - | >98% | |
| GC34557 | DIM-C-pPhCO2Me | 151358-48-4 | >99.50% | |
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist, with a K i value of 0.25μM. | ||||
| GC36292 | IDH1 Inhibitor 2 | 2244895-42-7 | >98% | |
IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM. | ||||
| GC36293 | IDH1 Inhibitor 3 | 2171081-24-4 | >98% | |
IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H. | ||||
| GC36665 | Mutant IDH1 inhibitor | 1429180-08-4 | >98.50% | |
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM. | ||||
| GC38640 | IDH889 | 1429179-07-6 | >98.50% | |
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM. | ||||
| GC39157 | DS-1001b | 1898207-64-1 | >98.50% | |
An inhibitor of mutant IDH1 | ||||
| GC50129 | TC-E 5008 | 50405-58-8 | >98% | |
Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal | ||||
| GC64359 | (R,R)-GSK321 | 1816272-19-1 | >99.00% | |
(R,R)-GSK321 is a mutant R132H IDH1 inhibitor with an IC 50 value of 120nM. | ||||
| GC65554 | IDH1 Inhibitor 1 | 2234285-81-3 | >99.00% | |
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity. | ||||
| GC65883 | (S,R)-WT IDH1 Inhibitor 2 | 1816272-18-0 | >98.00% | |
(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers. | ||||
