GSK321

  • Chemical Properties
CAS No. 1816331-63-1 Cat. No. BCP20143
Name GSK321
Synonyms GSK-321;GSK 321;
Formula C28H28FN5O3 M. Wt 501.22
  • Biological Activity
Description GSK321 is a potent and selective IDH1 mutant inhibitor. GSK321 potently inhibited intracellular 2-HG production in HT-1080 cells, with a half-maximal effective concentration (EC50) of 85 nM by LC/MS/MS analysis. The inhibition of mutant IDH1 by GSK321 overcomes the pathognomonic differentiation block of AML cells and induces myeloid differentiation of IDH1 mutant cells at the level of leukemic blasts and more stem-like cells.
Pathways Protease/Metabolic Enzyme 
Targets IDH 

Structure

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