GSK3685032

  • Chemical Properties
CAS No. 2170137-61-6 Cat. No. BCP43733
Name GSK3685032
Synonyms GSK-3685032;GSK 3685032;
Formula C22H24N6OS M. Wt 420.54
  • Biological Activity
Description GSK3685032, a potent first-in-class DNMT1-selective inhibitor that was shown via crystallographic studies to compete with the active-site loop of DNMT1 for penetration into hemi-methylated DNA between two CpG base pairs. GSK3685032 induces robust loss of DNA methylation, transcriptional activation and cancer cell growth inhibition in vitro. Due to improved in vivo tolerability compared with decitabine, GSK3685032 yields superior tumor regression and survival mouse models of acute myeloid leukemia.
Related Products GSK3685032TFA(GSK3685032 TFA ) 2170140-50-6((R)-GSK-3685032)
Pathways Epigenetics 
Targets DNA Methyltransferase 

Structure

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