2170140-50-6
Chemical Structure
(R)-GSK-3685032
- CAS No.: 2170140-50-6
- Formula:C22H24N6OS
- Molecular Weight:420.53
IUPAC Name: (R)-2-((6-(4-aminopiperidin-1-yl)-3,5-dicyano-4-ethylpyridin-2-yl)thio)-2-phenylacetamide
InChIKey: KNKHRZYILDZLRE-LJQANCHMSA-N
SMILES: N#CC1=C(N2CCC(CC2)N)N=C(C(C#N)=C1CC)S[C@H](C3=CC=CC=C3)C(N)=O
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].
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(R)-GSK-3685032 | 98.97% | (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. | ||||||||||||||||||||
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- [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. [Content Brief]
Keywords
