(R)-GSK-3685032

Names

[ Name ]:
(R)-GSK-3685032

Biological Activity

[Description]:

(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> DNA Methyltransferase

[Target]

DNMT1

[References]

[1]. Substituted pyridines as inhibitors of DNMT1 and their preparation. WO2017216727.

[2]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₄N₆OS

[ Molecular Weight ]:
420.53

Related Compounds

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