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Home >> Signaling Pathways >> Proteases >> Isocitrate Dehydrogenase (IDH)

Isocitrate Dehydrogenase (IDH)

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.

Targets for  Isocitrate Dehydrogenase (IDH)

Products for  Isocitrate Dehydrogenase (IDH)

  1. Cat.No. Product Name Information
  2. GC34417 (R,S)-Ivosidenib ((R,S)-AG-120) (R,S)-Ivosidenib ((R,S)-AG-120) Chemical Structure
  3. GC65883 (S,R)-WT IDH1 Inhibitor 2 (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. (S,R)-WT IDH1 Inhibitor 2 Chemical Structure
  4. GC67682 (S,S)-GSK321 (S,S)-GSK321 Chemical Structure
  5. GC15601 AG-120 AG-120 (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. AG-120 Chemical Structure
  6. GC13147 AG-221 (Enasidenib) AG-221 (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. AG-221 (Enasidenib) Chemical Structure
  7. GC10531 AGI-5198 A potent, selective inhibitor of IDH1 mutations AGI-5198 Chemical Structure
  8. GC14757 AGI-6780 A potent, selective inhibitor of mutant IDH2 AGI-6780 Chemical Structure
  9. GC19059 BAY-1436032 BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor. BAY-1436032 Chemical Structure
  10. GC39157 DS-1001b An inhibitor of mutant IDH1 DS-1001b Chemical Structure
  11. GC32904 Enasidenib mesylate (AG-221 mesylate) Enasidenib mesylate (AG-221 mesylate) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes. Enasidenib mesylate (AG-221 mesylate) Chemical Structure
  12. GC67771 GSK321 GSK321 Chemical Structure
  13. GC17809 GSK864 An inhibitor of mutant IDH1 GSK864 Chemical Structure
  14. GC65554 IDH1 Inhibitor 1 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. IDH1 Inhibitor 1 Chemical Structure
  15. GC36292 IDH1 Inhibitor 2 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. IDH1 Inhibitor 2 Chemical Structure
  16. GC36293 IDH1 Inhibitor 3 IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H. IDH1 Inhibitor 3 Chemical Structure
  17. GC18423 IDH305 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). IDH305 Chemical Structure
  18. GC38640 IDH889 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. IDH889 Chemical Structure
  19. GC36665 Mutant IDH1 inhibitor Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM. Mutant IDH1 inhibitor Chemical Structure
  20. GC10485 Mutant IDH1-IN-1 mutant IDH1 R132H inhibitor Mutant IDH1-IN-1 Chemical Structure
  21. GC32966 Mutant IDH1-IN-2 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. Mutant IDH1-IN-2 Chemical Structure
  22. GC33318 Mutant IDH1-IN-4 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. Mutant IDH1-IN-4 Chemical Structure
  23. GC31874 Olutasidenib (FT-2102) 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 . Olutasidenib (FT-2102) Chemical Structure
  24. GC50129 TC-E 5008 Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal TC-E 5008 Chemical Structure
  25. GC19380 Vorasidenib Vorasidenib is a pan isocitrate dehydrogenase (IDH) inhibitor. Vorasidenib Chemical Structure
  26. GC64359 WT IDH1 Inhibitor 2 WT IDH1 Inhibitor 2 (Compound 3) is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. WT IDH1 Inhibitor 2 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity. WT IDH1 Inhibitor 2 Chemical Structure

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