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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)

  • GC10485 structure
    GC10485Mutant IDH1-IN-1
    CAS: 1355326-21-4
    Purity: >99.50%

    mutant IDH1 R132H inhibitor

  • GC10531 structure
    GC10531AGI-5198
    CAS: 1355326-35-0
    Purity: >98.00%

    A potent, selective inhibitor of IDH1 mutations

  • GC13147 structure
    GC13147AG-221 (Enasidenib)
    CAS: 1446502-11-9
    Purity: >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 structure
    GC14757AGI-6780
    CAS: 1432660-47-3
    Purity: >98.00%

    AGI-6780 is an orally active, potent and selective mutant isocitrate dehydrogenase 2 (IDH2 R140Q ) inhibitor (IC₅₀=23±1.7nM).

  • GC15601 structure
    GC15601AG-120
    CAS: 1448347-49-6
    Purity: >98.00%

    AG-120 (Ivosidenib) is an inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1).

  • GC17809 structure
    GC17809GSK864
    CAS: 1816331-66-4
    Purity: >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 structure
    GC18423IDH305
    CAS: 1628805-46-8
    Purity: >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 structure
    GC19059BAY-1436032
    CAS: 1803274-65-8
    Purity: >99.00%

    BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

  • GC19380 structure
    GC19380Vorasidenib
    CAS: 1644545-52-7
    Purity: >99.50%

    Vorasidenib is a pan isocitrate dehydrogenase (IDH) inhibitor.

  • GC31874 structure
    GC31874Olutasidenib (FT-2102)
    CAS: 1887014-12-1
    Purity: >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 structure
    GC32904Enasidenib mesylate (AG-221 mesylate)
    CAS: 1650550-25-6
    Purity: >99.50%

    Enasidenib mesylate (AG-221 mesylate) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

  • GC32966 structure
    GC32966Mutant IDH1-IN-2
    CAS: 1429176-69-1
    Purity: >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 structure
    GC33318Mutant IDH1-IN-4
    CAS: 1416270-18-2
    Purity: >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 structure
  • GC34557 structure
    GC34557DIM-C-pPhCO2Me
    CAS: 151358-48-4
    Purity: >99.50%

    DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist, with a K i value of 0.25μM.

  • GC36292 structure
    GC36292IDH1 Inhibitor 2
    CAS: 2244895-42-7
    Purity: >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 structure
    GC36293IDH1 Inhibitor 3
    CAS: 2171081-24-4
    Purity: >98%

    IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H.

  • GC36665 structure
    GC36665Mutant IDH1 inhibitor
    CAS: 1429180-08-4
    Purity: >98.50%

    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

  • GC38640 structure
    GC38640IDH889
    CAS: 1429179-07-6
    Purity: >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 structure
    GC39157DS-1001b
    CAS: 1898207-64-1
    Purity: >98.50%

    An inhibitor of mutant IDH1

  • GC50129 structure
    GC50129TC-E 5008
    CAS: 50405-58-8
    Purity: >98%

    Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal

  • GC64359 structure
    GC64359(R,R)-GSK321
    CAS: 1816272-19-1
    Purity: >99.00%

    (R,R)-GSK321 is a mutant R132H IDH1 inhibitor with an IC 50 value of 120nM.

  • GC65554 structure
    GC65554IDH1 Inhibitor 1
    CAS: 2234285-81-3
    Purity: >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 structure
    GC65883(S,R)-WT IDH1 Inhibitor 2
    CAS: 1816272-18-0
    Purity: >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.