(R)-GSK-3685032 |
| Catalog No.GC64210 |
(R)-GSK-3685032 est l'énantiomère R de GSK-3685032. GSK-3685032 est un inhibiteur sélectif de la DNMT1 réversible, non dépendant du temps et non covalent, avec une IC50 de 0,036 μM. GSK-3685032 induit une perte robuste de méthylation de l'ADN, une activation de la transcription et une inhibition de la croissance des cellules cancéreuses.
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Cas No.: 2170140-50-6
Sample solution is provided at 25 µL, 10mM.
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(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].
[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.
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