Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-, (αR)-

Biological Activity

(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].

References

[1]. Adams, Nicholas David, et al. Substituted pyridines as inhibitors of DNMT1 and their preparation. WO2017216727A1. [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.