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

Isocitrate Dehydrogenase (IDH)(异柠檬酸脱氢酶)

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 for  Isocitrate Dehydrogenase (IDH)

  1. Cat.No. 产品名称 Information
  2. GC69254 IDH1 Inhibitor 7 IDH1 Inhibitor 7 (Compound 88) 是一种 IDH1 抑制剂，IC50 小于100 nM。
  3. GC67771 GSK321 GSK321 是突变异柠檬酸脱氢酶 1 (IDH1) 酶的有效抑制剂。GSK321 对突变的 IDH1 酶具有高抑制性和选择性。GSK321 可用于急性髓性白血病的研究。
  4. GC67682 (S,S)-GSK321 (S,S)-GSK321 是 GSK321 的 (S,S)-对映异构体。
  5. GC65883 (S,R)-WT IDH1 Inhibitor 2 (S,R)-WT IDH1 Inhibitor 2 (GSK321) 是一个有效的选择性突变型 IDH1 抑制剂，抑制 R132G、R132C、R132H 和 WT IDH1 的 IC50 值分别为 2.9、3.8、4.6 和 46 nM，选择性比 IDH2 高出 100 倍。(S,R)-WT IDH1 Inhibitor 2 诱导细胞内 2-HG 减少，髓细胞分化阻滞失效，在白血病母细胞和更不成熟的干细胞水平诱导粒细胞分化。(S,R)-WT IDH1 Inhibitor 2 可用于急性髓系白血病 (AML) 及其他癌症的研究。
  6. GC65554 IDH1 Inhibitor 1 IDH1 Inhibitor 1 是一种有效的，口服生物可利用的，脑渗透性，选择性突变 IDH1 抑制剂，抑制 IDH1R132H，IDH1R132C，和 IDH1WT，IC50 分别为 0.021 μM, 0.045 μM, 和 2.52 μM。具有抗肿瘤活性。
  7. GC64359 WT IDH1 Inhibitor 2

    WT IDH1 Inhibitor 2 (Compound 3) 是野生型异柠檬酸脱氢酶1 (WT IDH1) 抑制剂，IC50 值为120 nM。WT IDH1 Inhibitor 2 作为突变体 R132H IDH1 抑制剂，是 GSK321 的异构体，具有野生型交叉反应性。
  8. GC50129 TC-E 5008 Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal
  9. GC39157 DS-1001b An inhibitor of mutant IDH1
  10. GC38640 IDH889 IDH889 是一种可口服利用的，脑渗透性的，变构和突变特异性的异柠檬酸脱氢酶 (IDH1) 抑制剂。IDH889 对 IDH1 R132* 突变型具有高效选择性，对 IDH1R132H、IDH1R132C 和 IDH1wt 作用的 IC50 值分别为 0.02 μM, 0.072 μM 和 1.38 μM。IDH889 具有高效的细胞内 2-HG 水平抑制作用，其 IC50 值为 0.014 μM。
  11. GC36665 Mutant IDH1 inhibitor Mutant IDH1 inhibitor 是一个有效的突变型 IDH1 R132H 的抑制剂，IC50 值小于 72 nM。
  12. GC36293 IDH1 Inhibitor 3 IDH1 Inhibitor 3 (compound 6f) 是突变型的 IDH1 的抑制剂，其对IDH1R132H 的 IC50 值为 45 nM。
  13. GC36292 IDH1 Inhibitor 2 IDH1 Inhibitor 2 是有效的IDH1 抑制剂，通过对 His315的共价修饰发挥作用，其IC50 值为110 nM。
  14. GC34417 (R,S)-Ivosidenib ((R,S)-AG-120) (R,S)-Ivosidenib是一种异柠檬酸脱氢酶(IDH1)抑制剂。
  15. GC33318 Mutant IDH1-IN-4 MutantIDH1-IN-4(compound434)是一种突变型异柠檬酸脱氢酶1(IDH1)的抑制剂，其对R132H、HT1080和U87R132H细胞中的突变型IDH1的IC50值≤0.5μM。
  16. GC32966 Mutant IDH1-IN-2 MutantIDH1-IN-2是一种突变型异柠檬酸脱氢酶(IDH)蛋白抑制剂,在LS-MS生物化学检测中IC50值为<22nM,荧光生物化学检测中IC50值为16.6nM。
  17. GC32904 Enasidenib mesylate (AG-221 mesylate) An inhibitor of mutant IDH2
  18. GC31874 Olutasidenib (FT-2102) An inhibitor of mutant IDH1
  19. GC19380 Vorasidenib An inhibitor of mutant IDH1 and IDH2
  20. GC19059 BAY-1436032 An inhibitor of mutant IDH1
  21. GC18423 IDH305 A potent and selective inhibitor of mutant IDH1
  22. GC17809 GSK864 An inhibitor of mutant IDH1
  23. GC15601 AG-120 An IDH1 inhibitor
  24. GC13147 AG-221 (Enasidenib) An inhibitor of mutant IDH2
  25. GC10485 Mutant IDH1-IN-1 An inhibitor of mutant IDH1
  26. GC14757 AGI-6780 A potent, selective inhibitor of mutant IDH2
  27. GC10531 AGI-5198 A potent, selective inhibitor of IDH1 mutations

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